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inquiryProduct informations Product Name (2R)-4-Benzyl-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]morpholin-3-one CAS No.
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inquiry(2R)-4-Benzyl-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]morpholin-3-one CAS No.:287930-75-0 Name: (2R)-4-Benzyl-2-[(1R)-1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]morpholin-3-one
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inquiryAs a leading manufacturer and supplier of chemicals in China, DayangChem not only supply popular chemicals, but also DayangChem’s R&D center offer custom synthesis services. DayangChem can provide different quantities of custom synthesis
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inquiryOur company was built in 2009 with an ISO certificate.In the past 5 years, we have grown up as a famous fine chemicals supplier in China and we had established stable business relationships with Samsung,LG,Merck,Thermo Fisher Scientific and so on.O
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inquiry1. Guaranteed purity; 2. Large quantity in stock; 3. Largest manufacturer; 4. Best service after shipment with email; 5. High quality & competitive price; Appearance:White Crystalline Powder Storage:Store in sealed conta
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inquiryHanways chempharm is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The marketing department is located in Wuhan. We have two GMP facilities in Hubei Pr
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inquiry(2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONE CAS:287930-75-0 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemi
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inquiryHello, dear friend! I'm Hansen and Allen from China. Welcome to my lookchem mall! The following is a brief introduction of our company's products and services. If you are interested in our products, please contact us by emai
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inquiryHenan Wentao Chemical Product Co.,Ltd is Located in Zhengzhou High-tech Development Zone with import and export license, We passed ISO 9001:2008 as well, Henan Wentao has developed more than 1000 compounds, which are widely used in the fields of prod
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inquiryOur Services 1. New Molecules R&D 2. Own test center HPLC NMR GC LC-MS 3. API and Intermediates from China reputed manufacturers 4. Documents support COA MOA MSDS DMF open part Our advantages 1. Government awarded company. Top 100 enter
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inquiryA substitute for perfluorooctanoic acid, mainly used as a surfactant, dispersant, additive, etc Appearance:White solid or Colorless liquid Purity:99.3 % We will ship the goods in a timely manner as required We can provide relevant documents acc
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inquiryZibo Hangyu Biotechnology Development Co., Ltd is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemi
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inquiry(2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONEAppearance:White powder Storage:Store in well-closed container, protected from light and in cool & dry place. Package:according to customers' requirements Application:Cance
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inquiryProduct name: (R)-4-Benzyl-2-((R)-1-(3,5-Bis(Trifluoromethyl)phenyl)ethoxy)Morpholin-3-one CAS No.: 287930-75-0 Molecule Formula:C21H19F6NO3 Molecule Weight:No Purity: 99.0% Package: 25kg/drum Description:White powder Manufacture Stan
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inquiryProduct Details Grade: pharmaceutical grade Purity:99%+ ProductionCapacity: 1000 Kilogram/Month Scope of use: For scientific research only(The product must be used legally) Our Advantage 1. Best quality with competitive price. 2. Quick shipping,
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inquiryProduct Name: (2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONE Synonyms: (2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONE;(R)-4-benzyl-2-((R)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)M
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inquiryHangzhou Huarong Pharm Co., Ltd.established since 2006 , has been actively developing specialty products for Finished Dosages, APIs, Intermediates, and Fine chemicals markets in North America, Europe, Korea, Japan, Mid-East and all over the World. Hu
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inquiryShandong Mopai Biotechnology Co., LTD is a leading manufacturer and supplier of chemicals in China. We develop produce and distribute high quality pharmaceuticals, intermediates, special chemicals and OLED intermediates and other fine chemicals. W
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inquiryProduct Name: (2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONE Synonyms: (2R)-4-BENZYL-2-{(1R)-1-[3,5-BIS(TRIFLUOROMETHYL)PHENYL]ETHOXY}MORPHOLIN-3-ONE;(R)-4-benzyl-2-((R)-1-(3,5-bis(trifluoroMethyl)phenyl)ethoxy)Mor
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inquirySAGECHEM is a chemical R&D, manufacturing and distribution company in China since 2009, including pharmaceutical intermediates, agrochemical, dyestuff intermediates, organosilicone, API and etc. We also offer a full range of services in
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inquiryHigh quality,stable supply chain.Appearance:white/off-white or light yellow Storage:Store in cool and dry place, keep away from strong light and heat. Package:aluminum bottle,glass bottle,PTFE bottle,cardboard drum Application:This product can be use
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inquiryWe are a Union of chemistry in China, consists of chemists,engineers, laboratories,factories in China. We organize surplus capacity of R&D and production as well as custom synthesis for chemical products and chemical business project. We are supp
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inquiry1.High quality 2.High purity 3.Best price 4.Best service 5.Professional manufacturer 6.Loyal and honest supplier 7.Fast response to customer within 6 hours Application:Pharmaceutical Intermediate
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inquiryISO/factory/goodqualityAppearance:off white Storage:Dry,cool place Package:drum Application:active pharmaceutical ingredients Transportation:by air/sea/express Port:shenzhen/shanghai
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inquiry(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
4-benzyl-2-hydroxy-morpholin-3-one
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Stage #1: 4-benzyl-2-hydroxy-morpholin-3-one With trifluoroacetic anhydride In acetonitrile at 5 - 30℃; for 1h; Stage #2: (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol With boron trifluoride diethyl etherate In acetonitrile for 3h; Further stages; | 96% |
Stage #1: 4-benzyl-2-hydroxy-morpholin-3-one With trifluoroacetic anhydride In acetonitrile at 5 - 30℃; for 1h; Stage #2: (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol With boron trifluoride diethyl etherate In acetonitrile for 2h; Stage #3: With tetrahydrolinalool; potassium tert-butylate In hexane at -10 - -5℃; for 14h; Solvent; | 96% |
Stage #1: 4-benzyl-2-hydroxy-morpholin-3-one With trifluoroacetic anhydride In acetonitrile at 5℃; for 1h; Stage #2: (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol With boron trifluoride diethyl etherate In acetonitrile at 25℃; for 4h; Temperature; Reagent/catalyst; |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With di-chlorobenzyl azodicarboxylate; triphenylphosphine In dichloromethane at 10 - 20℃; for 12h; Concentration; Solvent; Reagent/catalyst; | 91.5% |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
2,2,2-trichloro-acetimidic acid 4-benzyl-3-oxo-morpholin-2-yl ester
B
(2S,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
C
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With boron trifluoride diethyl etherate In n-heptane; toluene at 20℃; for 1h; |
(2S,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With potassium tert-butylate In hexane; tert-butyl alcohol at 22℃; for 16h; |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
trifluoro-acetic acid 4-benzyl-3-oxo-morpholin-2-yl ester
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With boron trifluoride diethyl etherate In acetonitrile at 20℃; for 2h; | 3.51 kg |
Stage #1: (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol; trifluoro-acetic acid 4-benzyl-3-oxo-morpholin-2-yl ester With boron trifluoride diethyl etherate In acetonitrile at 25℃; Stage #2: With sodium hydroxide at 20℃; for 0.25h; Stage #3: With linalool potassium at 92℃; |
3,5-bis(trifluoromethyl)phenyl methyl ketone
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 3: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme | |
Multi-step reaction with 2 steps 1: 97 percent / borane-methyl sulfide complex; (S)-Me-CBS / various solvent(s); toluene / 1 h / -5 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: dimethylsulfide borane complex / tert-butyl methyl ether / 1 h / -10 - -5 °C / Inert atmosphere 2.1: trifluoroacetic anhydride / acetonitrile / 1 h / 25 °C / Inert atmosphere 2.2: 2 h / 20 - 30 °C View Scheme |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme |
4-benzyl-morpholine-2,3-dione
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 4: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme | |
Multi-step reaction with 3 steps 1: 80 percent / lithium tri(sec-butyl)borohydride; sodium hydroxide; hydrogen peroxide / tetrahydrofuran; H2O / 1 h / 10 °C 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C View Scheme |
N-Benzylethanolamine
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: acetonitrile / 5 - 34 °C 3: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 4: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme | |
Multi-step reaction with 3 steps 1: 76 percent / tetrahydrofuran; H2O / 21 h / Heating 2: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 3: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C View Scheme |
4-benzyl-2-hydroxy-morpholin-3-one
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: acetonitrile / 5 - 34 °C 2: 3.51 kg / BF3*Et2O / acetonitrile / 2 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 3: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme | |
Multi-step reaction with 2 steps 1: 91 percent / DBU / toluene; heptane / 18 h / 20 °C 2: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C View Scheme |
2,2,2-trichloro-acetimidic acid 4-benzyl-3-oxo-morpholin-2-yl ester
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: boron trifluoride etherate / toluene; heptane / 1 h / 20 °C 2: KO-t-Bu / 2-methyl-propan-2-ol; hexane / 16 h / 22 °C View Scheme |
4-benzyl-2-hydroxy-morpholin-3-one
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With potassium tetrahydrolinalool; triphenylphosphine at -10℃; for 6h; Reagent/catalyst; Temperature; | 80.2 g |
(R)-[3,5-bis(trifluoromethyl)phenyl]ethanol
4-benzyl-2-hydroxy-morpholin-3-one
A
(2S,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
B
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Stage #1: 4-benzyl-2-hydroxy-morpholin-3-one With trifluoroacetic anhydride In acetonitrile at 25℃; for 1h; Inert atmosphere; Stage #2: (R)-[3,5-bis(trifluoromethyl)phenyl]ethanol With boron trifluoride diethyl etherate In acetonitrile at 20 - 30℃; for 2h; stereoselective reaction; | A 39.5 g B 23.2 g |
N-Benzylethanolamine
A
(2S,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
B
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: water; tetrahydrofuran / 8 h / 60 - 65 °C / Inert atmosphere 2.1: trifluoroacetic anhydride / acetonitrile / 1 h / 25 °C / Inert atmosphere 2.2: 2 h / 20 - 30 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
With 5%-palladium/activated carbon; hydrogen In methanol; water at 50 - 60℃; under 26252.6 Torr; for 4.5h; | 99% |
4-flourophenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Stage #1: 4-flourophenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one In tetrahydrofuran; methanol at 15 - 20℃; for 0.916667h; Stage #2: With palladium 10% on activated carbon; ammonium formate; toluene-4-sulfonic acid In tetrahydrofuran; methanol Stage #3: With hydrogenchloride In di-isopropyl ether; water for 0.5h; Reflux; | 94.7% |
With hydrogenchloride; hydrogen; toluene-4-sulfonic acid; palladium on activated charcoal In tetrahydrofuran; methanol at 20 - 25℃; under 1034.32 Torr; for 3h; | 47.6 g |
Stage #1: 4-flourophenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one With toluene-4-sulfonic acid In tetrahydrofuran; methanol at 0 - 10℃; Stage #2: In methanol at 20 - 30℃; under 1034.32 Torr; for 4h; High pressure; |
1-Bromo-4-fluorobenzene
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Stage #1: 1-Bromo-4-fluorobenzene; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one With palladium on activated charcoal; hydrogen; magnesium In tetrahydrofuran Stage #2: With hydrogenchloride In tetrahydrofuran; water Reagent/catalyst; | 93.1% |
phenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
[2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-phenylmorpholine
Conditions | Yield |
---|---|
Stage #1: phenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one In tetrahydrofuran at 15 - 25℃; for 0.5h; Stage #2: With 5%-palladium/activated carbon; hydrogen; toluene-4-sulfonic acid In tetrahydrofuran; methanol at 10 - 35℃; under 258.581 Torr; for 4h; | 53% |
4-flourophenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
[2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine
Conditions | Yield |
---|---|
Stage #1: 4-flourophenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one In tetrahydrofuran at 20℃; Stage #2: With hydrogen; 5 percent Pd/C In methanol Further stages.; | |
Stage #1: 4-flourophenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one In tetrahydrofuran at 15 - 25℃; for 0.5h; Stage #2: With 5%-palladium/activated carbon; hydrogen; toluene-4-sulfonic acid In tetrahydrofuran; methanol at 0 - 25℃; under 1034.32 Torr; for 3h; |
4-flourophenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
B
[2R-[2α(R*),3α]]-2-[1-[3,5-bis(trifluoromethyl)phenyl]ethoxy]-3-(4-fluorophenyl)morpholine
Conditions | Yield |
---|---|
Stage #1: 4-flourophenylmagnesium bromide; (2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one In tetrahydrofuran at 20 - 30℃; Stage #2: With hydrogen; 10 percent Pd/C In tetrahydrofuran; methanol Further stages.; | A 5.96 g B n/a |
4-flourophenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
In tetrahydrofuran at 20℃; |
4-flourophenylmagnesium bromide
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
In tetrahydrofuran at 20℃; for 3h; | A 0.76 g B 0.96 g |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 2.1: NaHCO3 / ethyl acetate 2.2: 84 percent / K2CO3; N-chlorosuccinimide; DBU / toluene; dimethylformamide / 5 h / 20 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: tetrahydrofuran / 20 - 30 °C 1.2: 5.96 g / H2 / 10 percent Pd/C / methanol; tetrahydrofuran 2.1: K2CO3 / dimethylformamide / 120 h / 20 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: tetrahydrofuran / 20 - 30 °C 1.2: 5.96 g / H2 / 10 percent Pd/C / methanol; tetrahydrofuran 2.1: ethyl acetate; aq. NaHCO3 / 2 h / 20 °C 2.2: triehtylamine / CH2Cl2 / 2 h / 0 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
aprepitant
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr View Scheme | |
Multi-step reaction with 3 steps 1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 2: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C 3: 0.96 kg / Darco / methanol / 1 h / 60 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: 5%-palladium/activated carbon; hydrogen / methanol; water / 4.5 h / 50 - 60 °C / 26252.6 Torr 2.1: sodium hydroxide / acetonitrile / 2.5 h / 30 - 40 °C 3.1: tetrahydrofuran / 1 h / 15 - 25 °C 3.2: 1 h / 20 - 65 °C 4.1: triethylsilane; boron trifluoride diethyl etherate / acetonitrile / 5 h / 0 - 35 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
(2R,3R)-2-[(1R)-1-(3,5-bis-trifluoro-methylphenyl)ethoxy]-3-(4-fluorophenyl)morpholine
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: tetrahydrofuran / 20 - 30 °C 1.2: 5.96 g / H2 / 10 percent Pd/C / methanol; tetrahydrofuran 2.1: ethyl acetate; aq. NaHCO3 / 2 h / 20 °C 2.2: triehtylamine / CH2Cl2 / 2 h / 0 °C 3.1: 46 mg / triethylamine / acetonitrile / 20 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
2-(R)-(1-(R)-(3,5-bis(trifluoromethyl)phenyl)ethoxy)-3-(S)-4-fluorophenyl-4-2-(N-methylcarboxyactamidrazono)morpholine
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 47.6 g / 4-toluenesulfonic acid; H2; HCl / Pd/C / tetrahydrofuran; methanol / 3 h / 20 - 25 °C / 1034.32 Torr 2: potassium carbonate / toluene; dimethylsulfoxide / 2 h / 15 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: tetrahydrofuran / 0.5 h / 15 - 25 °C 1.2: 3 h / 0 - 25 °C / 1034.32 Torr 2.1: hydrogenchloride / water View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1.1: tetrahydrofuran / 0.5 h / 15 - 25 °C 1.2: 3 h / 0 - 25 °C / 1034.32 Torr 2.1: hydrogenchloride / water 3.1: potassium carbonate / N,N-dimethyl-formamide / 20 °C View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1.1: tetrahydrofuran / 0.5 h / 15 - 25 °C 1.2: 4 h / 10 - 35 °C / 258.58 Torr 2.1: hydrogenchloride / water View Scheme |
(2R,2αR)-4-benzyl-2-[1-[3,5-bis(trifluoromethyl)phenyl]]ethoxy-morpholin-3-one
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1.1: tetrahydrofuran / 0.5 h / 15 - 25 °C 1.2: 3 h / 0 - 25 °C / 1034.32 Torr 2.1: hydrogenchloride / water 3.1: potassium carbonate / N,N-dimethyl-formamide / 20 °C 4.1: hydrogenchloride / water View Scheme |
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