Product Name

  • Name

    Brinzolamide

  • EINECS 620-511-8
  • CAS No. 138890-62-7
  • Article Data11
  • CAS DataBase
  • Density 1.5 g/cm3
  • Solubility
  • Melting Point 130.0 to 134.0 °C
  • Formula C12H21N3O5S3
  • Boiling Point 586 °C at 760mmHg
  • Molecular Weight 383.514
  • Flash Point 308.2 °C
  • Transport Information
  • Appearance crystalline solid
  • Safety
  • Risk Codes R36/37/38
  • Molecular Structure Molecular Structure of 138890-62-7 (Brinzolamide)
  • Hazard Symbols Xi
  • Synonyms 2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide,4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)-;AL 4862;2H-Thieno[3,2-e]-1,2-thiazine-6-sulfonamide,4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (4R)-;Brinzolamide (JAN/USP);
  • PSA 163.80000
  • LogP 3.27760

Synthetic route

C21H29N3O8S4

C21H29N3O8S4

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With sodium thiomethoxide In methanol at 0 - 25℃; for 12h; Reagent/catalyst;83%
C21H29N5O9S4

C21H29N5O9S4

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With sodium tetradecyl mercaptan In methanol at 0 - 25℃; Reagent/catalyst;81%
C11H18N2O8S4

C11H18N2O8S4

ethylamine
75-04-7

ethylamine

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
In tetrahydrofuran; water at 0 - 30℃;66.3%
(R)-3,4-dihydro-4-ethylamino-6-chloro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide hydrochloride

(R)-3,4-dihydro-4-ethylamino-6-chloro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide hydrochloride

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Stage #1: (R)-3,4-dihydro-4-ethylamino-6-chloro-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide hydrochloride With sodium hydrogencarbonate
Stage #2: With n-butyllithium In tetrahydrofuran; hexane at -40℃; for 1h;		63%
C20H26N2O9S4

C20H26N2O9S4

ethylamine
75-04-7

ethylamine

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
In water at 11 - 20℃; for 15h; enantioselective reaction;61%
Stage #1: C20H26N2O9S4; ethylamine In water at 10 - 12℃; for 15h;
Stage #2: With hydrogenchloride In water at 20℃; for 1h; Temperature;		2.4 g
(R)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide
165117-54-4

(R)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide

ethylamine
75-04-7

ethylamine

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Stage #1: (R)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide With zinc(II) tosylate; triphenylphosphine; diethylazodicarboxylate In tetrahydrofuran at 20 - 80℃; for 8h;
Stage #2: ethylamine In tetrahydrofuran at 0 - 20℃; for 36h; Product distribution / selectivity;		49%
Stage #1: (R)-3,4-Dihydro-4-hydroxy-2-(3-methoxypropyl)-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide 1,1-dioxide With zinc(II) tosylate; triphenylphosphine; diethylazodicarboxylate In tetrahydrofuran at 20 - 80℃;
Stage #2: ethylamine In tetrahydrofuran at 0 - 20℃;
(S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide
154127-42-1

(S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide

ethylamine
75-04-7

ethylamine

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Stage #1: (S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide With toluene-4-sulfonic acid; triethylamine In tetrahydrofuran at 0 - 20℃; for 18h;
Stage #2: ethylamine In tetrahydrofuran at 0 - 20℃; for 36h;
Stage #1: (S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide With triethylamine; p-toluenesulfonyl chloride In tetrahydrofuran at 0 - 20℃; for 18h;
Stage #2: ethylamine In tetrahydrofuran at 0 - 20℃;
C12H19N2O5S3(1-)*Li(1+)

C12H19N2O5S3(1-)*Li(1+)

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With sodium acetate; hydroxylamine-O-sulfonic acid In hexane at 0 - 20℃; Product distribution / selectivity;
(R)-3,4-dihydro-4-(N-ethylamino)-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide
1029324-92-2

(R)-3,4-dihydro-4-(N-ethylamino)-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Stage #1: (R)-3,4-dihydro-4-(N-ethylamino)-2-(3-methoxy)propyl-2H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide With n-butyllithium In tetrahydrofuran; hexane at -60℃; for 8.75h; Inert atmosphere;
Stage #2: With sulfur dioxide In tetrahydrofuran; hexane at -65 - 20℃;
Stage #3: With sodium acetate trihydrate; hydroxylamine-O-sulfonic acid In ethyl acetate at 0 - 20℃;
brinzolamide

brinzolamide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With chiral-prep-HPLC (Chiralpak IA0.46x15 cm, 5 umChiral-A (IA)002IA00CD-LF007) Resolution of racemate;
(S)-3,4-dihydro-6-chloro-4-hydroxy-2-(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine 1,1-dioxide
160982-13-8

(S)-3,4-dihydro-6-chloro-4-hydroxy-2-(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine 1,1-dioxide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1.1: triethylamine / tetrahydrofuran / 0 - 20 °C
2.1: water; tetrahydrofuran / 0 - 20 °C
2.2: pH 1 - 3
3.1: sodium hydrogencarbonate
3.2: 1 h / -40 °C
View Scheme
Multi-step reaction with 4 steps
1.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
1.2: 20 °C / pH 4
1.3: 15 h / 0 - 25 °C
2.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
3.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
4.1: water / 15 h / 11 - 20 °C
View Scheme
C17H20ClNO6S3

C17H20ClNO6S3

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1.1: water; tetrahydrofuran / 0 - 20 °C
1.2: pH 1 - 3
2.1: sodium hydrogencarbonate
2.2: 1 h / -40 °C
View Scheme
(R)-(+)-4-ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide maleate
1448780-04-8

(R)-(+)-4-ethylamino-2-(3-methoxypropyl)-3,4-dihydro-2H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide maleate

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With triethylamine In water at 25 - 30℃; for 2h; pH=7 - 8.5;45 g
Brinzolamide hydrochloride
150937-43-2

Brinzolamide hydrochloride

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With triethylamine In water at 25 - 30℃; for 2h; pH=7 - 8.5;500 g
C13H20N2O7S3

C13H20N2O7S3

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 2 steps
1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
2: water / 15 h / 11 - 20 °C
View Scheme
Multi-step reaction with 2 steps
1: triphenylphosphine; di-isopropyl azodicarboxylate / dichloromethane / 15 h / 0 - 20 °C / Inert atmosphere
2: sodium thiomethoxide / methanol / 12 h / 0 - 25 °C
View Scheme
3-acetyl-5-chloro-2-thiophenesulfenamide

3-acetyl-5-chloro-2-thiophenesulfenamide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 8 steps
1.1: sodium tungstate (VI) dihydrate; dihydrogen peroxide / water / 19 h / 15 - 35 °C
2.1: pyridinium hydrobromide perbromide; sulfuric acid / ethyl acetate / 1.5 h / 1 - 5 °C / Large scale
3.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
3.2: 2 h / 0 - 22 °C
4.1: potassium carbonate / dimethyl sulfoxide
5.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
5.2: 20 °C / pH 4
5.3: 15 h / 0 - 25 °C
6.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
7.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
8.1: water / 15 h / 11 - 20 °C
View Scheme
3-acetyl-5-chloro-2-thiophenesulfonamide

3-acetyl-5-chloro-2-thiophenesulfonamide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 7 steps
1.1: pyridinium hydrobromide perbromide; sulfuric acid / ethyl acetate / 1.5 h / 1 - 5 °C / Large scale
2.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
2.2: 2 h / 0 - 22 °C
3.1: potassium carbonate / dimethyl sulfoxide
4.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
4.2: 20 °C / pH 4
4.3: 15 h / 0 - 25 °C
5.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
6.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
7.1: water / 15 h / 11 - 20 °C
View Scheme
3-(2-Bromoacetyl)-5-chloro-thiophene-2-sulfonamide

3-(2-Bromoacetyl)-5-chloro-thiophene-2-sulfonamide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 6 steps
1.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
1.2: 2 h / 0 - 22 °C
2.1: potassium carbonate / dimethyl sulfoxide
3.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
3.2: 20 °C / pH 4
3.3: 15 h / 0 - 25 °C
4.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
5.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
6.1: water / 15 h / 11 - 20 °C
View Scheme
3-acetyl-2,5-dichlorothiophene
36157-40-1

3-acetyl-2,5-dichlorothiophene

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 11 steps
1.1: thiourea / ethanol; water / 2 h / Reflux; Large scale
1.2: 3 h / Reflux; Large scale
2.1: chlorine / toluene / 0.42 h / 8 °C / Cooling with ice
3.1: ammonia / 1 h / 5 - 15 °C
4.1: sodium tungstate (VI) dihydrate; dihydrogen peroxide / water / 19 h / 15 - 35 °C
5.1: pyridinium hydrobromide perbromide; sulfuric acid / ethyl acetate / 1.5 h / 1 - 5 °C / Large scale
6.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
6.2: 2 h / 0 - 22 °C
7.1: potassium carbonate / dimethyl sulfoxide
8.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
8.2: 20 °C / pH 4
8.3: 15 h / 0 - 25 °C
9.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
10.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
11.1: water / 15 h / 11 - 20 °C
View Scheme
(S)-3,4-dihydro-6-chloro-4-hydroxy-4H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide

(S)-3,4-dihydro-6-chloro-4-hydroxy-4H-thieno[3,2-e]-1,2-thiazine-1,1-dioxide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 5 steps
1.1: potassium carbonate / dimethyl sulfoxide
2.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
2.2: 20 °C / pH 4
2.3: 15 h / 0 - 25 °C
3.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
4.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
5.1: water / 15 h / 11 - 20 °C
View Scheme
3-Acetyl-2-(phenylmethyl)thio-5-chlorothiophene
160982-09-2

3-Acetyl-2-(phenylmethyl)thio-5-chlorothiophene

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 10 steps
1.1: chlorine / toluene / 0.42 h / 8 °C / Cooling with ice
2.1: ammonia / 1 h / 5 - 15 °C
3.1: sodium tungstate (VI) dihydrate; dihydrogen peroxide / water / 19 h / 15 - 35 °C
4.1: pyridinium hydrobromide perbromide; sulfuric acid / ethyl acetate / 1.5 h / 1 - 5 °C / Large scale
5.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
5.2: 2 h / 0 - 22 °C
6.1: potassium carbonate / dimethyl sulfoxide
7.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
7.2: 20 °C / pH 4
7.3: 15 h / 0 - 25 °C
8.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
9.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
10.1: water / 15 h / 11 - 20 °C
View Scheme
(S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide
154127-42-1

(S)-3,4-dihydro-4-hydroxy-2(3-methoxypropyl)-4H-thieno[3,2-e]-1,2-thiazine-6-sulfonamide-1,1-dioxide

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 3 steps
1: acetonitrile / 19 h / 30 - 85 °C / Reflux
2: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
3: water / 15 h / 11 - 20 °C
View Scheme
Multi-step reaction with 3 steps
1.1: triethylamine / acetonitrile / 5 h / 78 °C
2.1: triethylamine / tetrahydrofuran / 3 h / -10 - -4 °C
3.1: water / 15 h / 10 - 12 °C
3.2: 1 h / 20 °C
View Scheme
Multi-step reaction with 3 steps
1: acetonitrile / 1 h / 5 - 15 °C / Inert atmosphere
2: triphenylphosphine; di-isopropyl azodicarboxylate / ethyl acetate / 15 h / 0 - 20 °C / Inert atmosphere
3: sodium tetradecyl mercaptan / methanol / 0 - 25 °C
View Scheme
Multi-step reaction with 3 steps
1: acetonitrile / 1 h / 5 - 15 °C / Inert atmosphere
2: triphenylphosphine; di-isopropyl azodicarboxylate / dichloromethane / 15 h / 0 - 20 °C / Inert atmosphere
3: sodium thiomethoxide / methanol / 12 h / 0 - 25 °C
View Scheme
3-acetyl-5-chloro-2-thiophenesulfenyl chloride

3-acetyl-5-chloro-2-thiophenesulfenyl chloride

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
Multi-step reaction with 9 steps
1.1: ammonia / 1 h / 5 - 15 °C
2.1: sodium tungstate (VI) dihydrate; dihydrogen peroxide / water / 19 h / 15 - 35 °C
3.1: pyridinium hydrobromide perbromide; sulfuric acid / ethyl acetate / 1.5 h / 1 - 5 °C / Large scale
4.1: B-chlorodiisopinocampheylborane / tert-butyl methyl ether / 3.5 h / -40 - -32 °C / Inert atmosphere
4.2: 2 h / 0 - 22 °C
5.1: potassium carbonate / dimethyl sulfoxide
6.1: n-butyllithium / hexane; tetrahydrofuran / 3.5 h / -70 - -66 °C / Inert atmosphere
6.2: 20 °C / pH 4
6.3: 15 h / 0 - 25 °C
7.1: acetonitrile / 19 h / 30 - 85 °C / Reflux
8.1: triethylamine / tetrahydrofuran / 2 h / -10 - -2 °C / Inert atmosphere
9.1: water / 15 h / 11 - 20 °C
View Scheme
brinzolamide

brinzolamide

A

(S)-brinzolamide

(S)-brinzolamide

B

brinzolamide
138890-62-7

brinzolamide

Conditions
ConditionsYield
With AmyCoat [tris(3,5-dimethylphenylcarbamate)amylose] (150 x 46 mm id) chiral column In hexane; isopropyl alcohol at 25℃; Reagent/catalyst; Resolution of racemate;
(S)-2-[(1,1-dimethylethyl)diphenylsilyl]oxypropanoic acid
125941-75-5

(S)-2-[(1,1-dimethylethyl)diphenylsilyl]oxypropanoic acid

brinzolamide
138890-62-7

brinzolamide

(2S)-2-[(tert-butyldiphenylsilyl)oxy]-N-{[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}propanamide

(2S)-2-[(tert-butyldiphenylsilyl)oxy]-N-{[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}propanamide

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;76%
(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

brinzolamide
138890-62-7

brinzolamide

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;76%
(2S)-2-{[(2S)-2-{[(2S)-2-(acetyloxy)propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-(acetyloxy)propanoyl]oxy}propanoyl]oxy}propanoic acid

brinzolamide
138890-62-7

brinzolamide

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;75%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

brinzolamide
138890-62-7

brinzolamide

C64H87N3O29S3Si

C64H87N3O29S3Si

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;74%
(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester

(S)-2-(tert-butyldiphenylsilanyloxy)propionic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester

brinzolamide
138890-62-7

brinzolamide

C43H59N3O15S3Si

C43H59N3O15S3Si

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;68.6%
brinzolamide
138890-62-7

brinzolamide

(R)-4-(ethylamino)-2-(3-hydroxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide1,1-dioxide
186377-56-0

(R)-4-(ethylamino)-2-(3-hydroxypropyl)-3,4-dihydro-2H-thieno[3,2-e][1,2]thiazine-6-sulfonamide1,1-dioxide

Conditions
ConditionsYield
With boron tribromide In dichloromethane at -78 - 25℃; for 24.1667h; Inert atmosphere;66%
Stage #1: brinzolamide With boron tribromide In dichloromethane at -78 - 20℃; for 24.16h;
Stage #2: With hydrogenchloride In water; dimethyl sulfoxide		66%
(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-carboxy-ethyl ester

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-carboxy-ethyl ester

brinzolamide
138890-62-7

brinzolamide

(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethyl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethyl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;65%
(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

(S)-2-(tert-butyl-diphenyl-silanyloxy)-propionic acid (S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)-ethoxycarbonyl]-ethyl ester

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-[(tert-butyldiphenylsilyl)oxy]propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;65%
succinic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester 3-[1-[4-(2-diethylaminoethylcarbamoyl)-3,5-dimethyl-1H-pyrrol-2-yl]-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl ester

succinic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethyl ester 3-[1-[4-(2-diethylaminoethylcarbamoyl)-3,5-dimethyl-1H-pyrrol-2-yl]-meth-(Z)-ylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl ester

brinzolamide
138890-62-7

brinzolamide

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

Conditions
ConditionsYield
With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 2h; Inert atmosphere;46%
(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-{[(2S)-2-[(tert butyldiphenylsilyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoyl]oxy}propanoic acid

brinzolamide
138890-62-7

brinzolamide

C58H79N3O25S3Si

C58H79N3O25S3Si

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;44.3%
(2S)‐2‐{[(2S)‐2‐(acetyloxy)propanoyl]oxy}propanoic acid

(2S)‐2‐{[(2S)‐2‐(acetyloxy)propanoyl]oxy}propanoic acid

brinzolamide
138890-62-7

brinzolamide

(S)-2-acetoxypropionic acid (S)-2-[4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ*6*-thieno[3,2-e][1,2]thiazine-6-sulfonylamino]-1-methyl-2-oxoethyl ester

(S)-2-acetoxypropionic acid (S)-2-[4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ*6*-thieno[3,2-e][1,2]thiazine-6-sulfonylamino]-1-methyl-2-oxoethyl ester

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;37%
octadecanoic acid (S)-1-[(S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethyl ester

octadecanoic acid (S)-1-[(S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-carboxy-ethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethyl ester

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl octadecanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl octadecanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;35%
(S)-2-[(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionyloxy]-propionic acid

(S)-2-[(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionyloxy]-propionic acid

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;32%
octadecanoic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxy carbonyl]ethoxycarbonyl}ethyl ester

octadecanoic acid (S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxy carbonyl]ethoxycarbonyl}ethyl ester

brinzolamide
138890-62-7

brinzolamide

octadecanoic acid (S)-1-[(S)-1-((S)-1-{(S)-2-[4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ*6*-thieno[3,2-e][1,2]thiazine-6-sulfonylamino]-1-methyl-2-oxo-ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethyl ester

octadecanoic acid (S)-1-[(S)-1-((S)-1-{(S)-2-[4-ethylamino-2-(3-methoxypropyl)-1,1-dioxo-1,2,3,4-tetrahydro-1λ*6*-thieno[3,2-e][1,2]thiazine-6-sulfonylamino]-1-methyl-2-oxo-ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethyl ester

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;27.3%
(S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionic acid

(S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionic acid

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl (2S)-2-(acetyloxy)propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;27%
(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionic acid

(S)-2-((S)-2-{(S)-2-[(S)-2-((S)-2-acetoxypropionyloxy)propionyloxy]propionyloxy}propionyloxy)propionic acid

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl(acetyloxy) propanoate

(2S)-1-{[(2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl(acetyloxy) propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;26%
(2S)-2-{[(2S)-2-{[(2S)-2-[(4-{[(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl]oxy}-4-oxobutanoyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoic acid

(2S)-2-{[(2S)-2-{[(2S)-2-[(4-{[(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2-yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl]oxy}-4-oxobutanoyl)oxy]propanoyl]oxy}propanoyl]oxy}propanoic acid

brinzolamide
138890-62-7

brinzolamide

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

(3Z)-3-[(4-{[2-(diethylamino)ethyl]carbamoyl}-3,5-dimethyl-1H-pyrrol-2yl)methylidene]-2-oxo-2,3-dihydro-1H-indol-5-yl (2S)-1-{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl butanedioate

Conditions
ConditionsYield
With dmap; benzotriazol-1-ol; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 2h; Inert atmosphere;26%
octadecanoic acid (S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethyl ester

octadecanoic acid (S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-{(S)-1-[(S)-1-((S)-1-carboxyethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethoxycarbonyl]ethoxycarbonyl}ethoxycarbonyl)ethyl ester

brinzolamide
138890-62-7

brinzolamide

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1{[(2S)-1-{[(2S)-1{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl octadecanoate

(2S)-1-{[(2S)-1-{[(2S)-1-{[(2S)-1{[(2S)-1-{[(2S)-1{[(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-c][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl]oxy}-1-oxopropan-2-yl octadecanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;25%
(S)-2-tert-butoxypropionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

(S)-2-tert-butoxypropionic acid (S)-1-((S)-1-carboxyethoxycarbonyl)ethyl ester

brinzolamide
138890-62-7

brinzolamide

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-(tert-butoxy)propanoate

(2S)-1-[(1S)-1-({[(4R)-4-(ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-2H,3H,4H-1λ6-thieno[3,2-e][1,2]thiazin-6-yl]sulfonyl}carbamoyl)ethoxy]-1-oxopropan-2-yl (2S)-2-(tert-butoxy)propanoate

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;24%
C54H84O26

C54H84O26

brinzolamide
138890-62-7

brinzolamide

C66H103N3O30S3

C66H103N3O30S3

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h;19.4%
C60H92O30

C60H92O30

brinzolamide
138890-62-7

brinzolamide

C72H111N3O34S3

C72H111N3O34S3

Conditions
ConditionsYield
With dmap; 1-ethyl-(3-(3-dimethylamino)propyl)-carbodiimide hydrochloride In dichloromethane at 0 - 30℃; for 1h; Inert atmosphere;8%

Brinzolamide Chemical Properties

Molecule structure of Brinzolamide (CAS NO.138890-62-7):

IUPAC Name: (4R)-4-(Ethylamino)-2-(3-methoxypropyl)-1,1-dioxo-3,4-dihydrothieno[3,2-e]thiazine-6-sulfonamide 
Molecular Weight: 383.50724 g/mol
Molecular Formula: C12H21N3O5S3 
Density: 1.5 g/cm3 
Boiling Point: 586 °C at 760 mmHg 
Flash Point: 308.2 °C
Index of Refraction: 1.625
Molar Refractivity: 90.39 cm3
Molar Volume: 255.3 cm3
Surface Tension: 69.7 dyne/cm 
Enthalpy of Vaporization: 87.53 kJ/mol
Vapour Pressure: 1.03E-13 mmHg at 25 °C
XLogP3-AA: -0.3
H-Bond Donor: 2
H-Bond Acceptor: 8
Rotatable Bond Count: 7
Exact Mass: 383.064333
MonoIsotopic Mass: 383.064333
Topological Polar Surface Area: 119
Heavy Atom Count: 23
Canonical SMILES: CCNC1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
Isomeric SMILES: CCN[C@H]1CN(S(=O)(=O)C2=C1C=C(S2)S(=O)(=O)N)CCCOC
InChI: InChI=1S/C12H21N3O5S3/c1-3-14-10-8-15(5-4-6-20-2)23(18,19)12-9(10)7-11(21-12)22(13,16)17/h7,10,14H,3-6,8H2,1-2H3,(H2,13,16,17)/t10-/m0/s1
InChIKey: HCRKCZRJWPKOAR-JTQLQIEISA-N
Product Categories: Chiral Reagents;Intermediates & Fine Chemicals;Pharmaceuticals

Brinzolamide Uses

 Brinzolamide (CAS NO.138890-62-7) is used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension.

Brinzolamide Specification

 Brinzolamide (CAS NO.138890-62-7) is also named as (R)-4-(Ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno(3,2-e)-1,2-thiazine-6-sulfonamide 1,1-dioxide ; (R)-4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-2H-thieno(3,2-e)-1,2-thiazine-6-sulfonamide ; 2H-Thieno(3,2-e)-1,2-thiazine-6-sulfonamide, 4-(ethylamino)-3,4-dihydro-2-(3-methoxypropyl)-, 1,1-dioxide, (R)- ; AL 4862 ; Azopt ; UNII-9451Z89515 . Brinzolamide (CAS NO.138890-62-7) is crystalline solid. It is a carbonic anhydrase inhibitor.

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