We are the manufacturer of this product in China. Our price is the lowest in China. CHANGZHOU HANGYU PHARMACEUTICAL TECHNOLOGY CO., LTD., founded in 1984, engages in pharmaceutical research, development, production, process design and techni
Cas:150683-30-0
Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquirySleeping pills and stability.This product is white or white crystalline powder;Odourless and slightly bitter taste.Almost insoluble in water, soluble in hydrochloric acid.In acid or alkali and heat hydrolysis, oral drug under the action of gastric
Cas:150683-30-0
Min.Order:10000 Gram
FOB Price: $1300.0
Type:Manufacturers
inquiryTolvaptan[CAS:150683-30-0] 7-Chloro-1,2,3,4-Tetrahydrobenzo[b]Azepin-5-one[CAS:160129-45-3] Items Specifications Results Appearance: light yellow or green crystalline powder Complies Solubil
Cas:150683-30-0
Min.Order:1 Kilogram
Negotiable
Type:Other
inquiryThe above product is Ality Chemical's strong item with best price, good quality and fast supply. Ality Chemical has been focusing on the research and production of this field for over 14 years. At the same time, we are always committed to providi
1. Factory price and high quality must be guaranteed, base on 8 years of production and R&D experience2. Free samples will be provided,ensure specifications and quality are right for customer3. Customers will receive the most professional technical s
Cas:150683-30-0
Min.Order:1 Gram
FOB Price: $0.1
Type:Manufacturers
inquiryShanghai Seasonsgreen Chemical is a high-tech research and development, production, sale and custom synthesis set in one high-tech chemical products enterprises. Our sales and marketing division is located in Shanghai, serving international pharmaceu
Cas:150683-30-0
Min.Order:1 Kilogram
FOB Price: $1.0
Type:Manufacturers
inquiryOur main production base is located in Xuzhou industry park. We are certified both to the ISO 9001 and ISO 14001 Standards, have a safety management system in place.Our R&D team masters core technology for process-design of target building block
Why is SINOWAY: 1) Specialized in pharmaceutical and healthcare industrial for 34 years. 2) ISO 9001:2015 & SGS audited supplier . 3) Accept various payment terms : T.T 30-60 days. 4) We have warehouse in USA with quickly shipment . 5) We c
Cas:150683-30-0
Min.Order:1 Kilogram
FOB Price: $100.0
Type:Trading Company
inquiryHenan Tianfu Chemical Co., Ltd. is located in Zhengzhou High-tech Development Zone with import and export license. We passed ISO 9001:2008 in 2009, and won "High-tech Enterprise" by provincial government in 2013.The objective of the com
Cas:150683-30-0
Min.Order:1 Kilogram
FOB Price: $1000.0
Type:Lab/Research institutions
inquiryOur advantages: 1, High quality with competitive price: 1) Standard:BP/USP/EP/Enterprise standard 2) All Purity≥99% 3) We are manufacturer and can provide high quality products with factory price. 2, Fast and safe delivery 1) Parcel can be
Cas:150683-30-0
Min.Order:1 Gram
FOB Price: $108.0 / 138.0
Type:Trading Company
inquiryOur Advantage: high quality with competitive price High quality standard: BP/USP/EP Enterprise standard All purity customized Fast and safe delivery We have reliable forwarder who can help us deliver our goods more fast and safe. We
Cas:150683-30-0
Min.Order:10 Kilogram
Negotiable
Type:Trading Company
inquiryAdvantage : LIDE PHARMACEUTICALS LTD. is a mid-small manufacturing-type enterprise, engaged in pharmaceutical intermediates of R&D, custom-made and production, and also involving trading chemicals for export. We have established the R&
Cas:150683-30-0
Min.Order:0
Negotiable
Type:Lab/Research institutions
inquiryProduct: Tolvaptan CAS: 150683-30-0 Molecular Formula: C26H25CLN2O3 Assay:99.0% min Appearacne: White powder Appearance:White powder Storage:Store in cool and dry place, away from sun light. Package:drum Application:pharmaceutical
1. 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
Cas:150683-30-0
Min.Order:10 Gram
Negotiable
Type:Other
inquiry1.No Less 8 years exporting experience. Clients can 100% received goods 2.Lower Price with higher quality 3,Free sample 4,We are sincerely responsible for the "product quality" and "After Service" Upbio is Specialized
Cas:150683-30-0
Min.Order:1 Kilogram
Negotiable
Type:Lab/Research institutions
inquiryOur company has been in existence for 10 years since its establishment. We have our own unique team. The company integrates independent research and development, production and sales. We have established famous brands at home and abroad. At present
Cas:150683-30-0
Min.Order:50 Gram
FOB Price: $576.0 / 630.0
Type:Trading Company
inquiryTolvaptan CAS:150683-30-0 Qingdao Belugas Import and Export Co., Ltd. is a scientific and technological company integrating research and development, production and trade of chemical intermediates, specializing in high quality organic intermediates,
Cas:150683-30-0
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
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
Henan 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
Product Name: Tolvaptan Synonyms: Tolvaptan powder;Tolvptan;(R)-N-(4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1H-benzo[b]azepine-1-carbonyl)-3-methylphenyl)-2-methylbenzamide;N-[4-(7-chloro-5-hydroxy-2,3,4,5-tetrahydro-1-benzazepine-1-carbonyl)-3-
Cas:150683-30-0
Min.Order:100 Gram
Negotiable
Type:Lab/Research institutions
inquiryAppearance:white powder without visible impurities Storage:Store in a cool,dry place and keep away from direct strong light Package:As customer request Application:Used for research and industrial manufacture. Transportation:By
Wuhan hanweishi Pharmchem Co., Ltd(Hanways chempharm) is a specialized company concentrating on the R&D, production, marketing and technical service of APIs and pharmaceutical intermediates. The leading products range are APIs, Hormones, Peptides
Cas:150683-30-0
Min.Order:100 Kilogram
Negotiable
Type:Trading Company
inquiry≥98.0% min Appearance:A white or off-white crystalline powder Storage:Room temperature Package:25kg/drum or as required Application:used in medicine Transportation:by sea by air express Port:China main port
Cas:150683-30-0
Min.Order:5 Kilogram
Negotiable
Type:Trading Company
inquiryOur company provides one-stop services of research - development - production for a variety of special prouducts. Not only do we make effective use of our strong technological strength, but also establish of cooperative relations with several well-
Cas:150683-30-0
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryJ&H CHEM R&D center can offer custom synthesis according to the contract research and development services for the fine chemicals, pharmaceutical, biotechnique and some of the other chemicals. J&H CHEM has some Manufacturing base in Jia
Zibo 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
Cas:150683-30-0
Min.Order:10 Gram
FOB Price: $100.0
Type:Lab/Research institutions
inquirymoderate price & quick delivery. Appearance:White Solid Storage:Stored in cool, dry and ventilation place; Away from fire and heat Package:100g/bottle,1kg/bottle,25kg/drum or as per your request Application:Tolvaptan (OPC-41061) is a select
Product name: Tolvaptan CAS No.:150683-30-0 Molecule Formula:C26H25ClN2O3 Molecule Weight:448.94 Purity: 99.0% Package: 25kg/drum Description:White powder Manufacture Standards:Enterprise Standard TESTING ITEMS
Product 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,
Cas:150683-30-0
Min.Order:1 Gram
Negotiable
Type:Lab/Research institutions
inquiryOur Advantages A. International Top level TechnologyOur company owned biomedicine experts are famous at home and abroad with rich experience in research and development in the field of efficient chiral functional molecules research and development an
MOP-21826
tolvaptan
Conditions | Yield |
---|---|
With methanol; sodium tetrahydroborate at 0℃; for 2h; | 96% |
With methanol; sodium tetrahydroborate at 20℃; for 5h; | 94% |
With sodium bis(2-methoxyethoxy)aluminium dihydride In tetrahydrofuran at -5 - 20℃; Solvent; | 94.2% |
MOP-21826
E
tolvaptan
Conditions | Yield |
---|---|
Stage #1: MOP-21826 With sodium tetrahydroborate In methanol for 1h; Stage #2: With hydrogenchloride In methanol; water at 20℃; | A n/a B n/a C n/a D n/a E 90% |
2-methyl-4-(2-methylbenzoylamino)benzoic acid chloride
tolvaptan
Conditions | Yield |
---|---|
With 2,6-dimethylpyridine In N,N-dimethyl acetamide; water at 0℃; for 2h; Reagent/catalyst; | 72% |
tolvaptan
Conditions | Yield |
---|---|
With sodium hydroxide In ethanol; water at 50℃; for 2h; | |
With sodium hydroxide; ethanol; water at 50℃; for 2h; |
(rac)-7-chloro-4-oxo-1,2,3,4-tetrahydronaphthalen-1-yl pivalate
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: 96 percent / hydroxylamine hydrochloride; sodium acetate / ethanol; H2O / 2 h / Heating 2: PCl5 / CH2Cl2 / 2 h / 20 °C 3: acetic acid; Zn / 0.5 h / Heating 4: BH3*THF / tetrahydrofuran / 0.5 h / Heating 5: 98 percent / triethylamine / CH2Cl2 / 1 h / 20 °C 6: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 7: triethylamine / CH2Cl2 / 1 h / 20 °C 8: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
2,2-dimethylpropionic acid 7-chloro-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl ester
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 98 percent / triethylamine / CH2Cl2 / 1 h / 20 °C 2: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 3: triethylamine / CH2Cl2 / 1 h / 20 °C 4: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: BH3*THF / tetrahydrofuran / 0.5 h / Heating 2: 98 percent / triethylamine / CH2Cl2 / 1 h / 20 °C 3: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 4: triethylamine / CH2Cl2 / 1 h / 20 °C 5: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
2,2-dimethylpropionic acid 4-[(E)-hydroxyimino]-7-chloro-1,2,3,4-tetrahydronaphthalen-1-yl ester
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: PCl5 / CH2Cl2 / 2 h / 20 °C 2: acetic acid; Zn / 0.5 h / Heating 3: BH3*THF / tetrahydrofuran / 0.5 h / Heating 4: 98 percent / triethylamine / CH2Cl2 / 1 h / 20 °C 5: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 6: triethylamine / CH2Cl2 / 1 h / 20 °C 7: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: acetic acid; Zn / 0.5 h / Heating 2: BH3*THF / tetrahydrofuran / 0.5 h / Heating 3: 98 percent / triethylamine / CH2Cl2 / 1 h / 20 °C 4: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 5: triethylamine / CH2Cl2 / 1 h / 20 °C 6: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
2,2-dimethylpropionic acid 7-chloro-1-(4-amino-2-methylbenzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl ester
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: triethylamine / CH2Cl2 / 1 h / 20 °C 2: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
2,2-dimethylpropionic acid 7-chloro-1-(2-methyl-4-nitrobenzoyl)-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl ester
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 82 percent / hydrochloric acid; SnCl2 / ethanol / 2 h / Heating 2: triethylamine / CH2Cl2 / 1 h / 20 °C 3: NaOH / ethanol; H2O / 2 h / 50 °C View Scheme |
4-chlorobenzenesulfonyl chloride
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1.1: 85 percent / pyridine / 20 °C 2.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 3.1: t-BuOK / toluene / 0.5 h / Heating 3.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 4.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 5.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 6.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 7.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 8.1: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme | |
Multi-step reaction with 7 steps 1: sodium carbonate / acetonitrile / 5 h / 80 °C 2: N-ethyl-N,N-diisopropylamine / dichloromethane / 4 h / 20 °C 3: potassium tert-butylate / toluene / 1 h / 120 °C 4: acetic acid; hydrogenchloride / water / 6 h / 100 °C 5: hydrogenchloride; tin(II) chloride dihdyrate / ethanol / 4 h / 20 °C 6: N-ethyl-N,N-diisopropylamine / dichloromethane / 2 h / 20 °C 7: sodium tetrahydroborate; methanol / 2 h / 0 °C View Scheme |
5-chloro-2-nitrobenzoic acid
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 10 steps 1.1: 100 percent / K2CO3 / acetone / 0.5 h / Heating 2.1: SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3.1: 85 percent / pyridine / 20 °C 4.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 5.1: t-BuOK / toluene / 0.5 h / Heating 5.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 6.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 7.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 8.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 9.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 10.1: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
2-methyl-4-nitrobenzoyl chloride
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 2: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 4: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: sodium hydrogencarbonate / dichloromethane; water / pH 7 - 8 2.1: tin(ll) chloride / methanol / 16 h / 20 °C 3.1: sodium hydrogencarbonate / dichloromethane / 0 - 5 °C / pH 7 - 8 4.1: sodium tetrahydroborate; methanol / 1 h / 20 °C 4.2: pH 6 - 7 View Scheme | |
Multi-step reaction with 4 steps 1.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 2.1: tin(IV) chloride / methanol / 16 h / 20 °C 3.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 4.1: sodium tetrahydroborate / methanol / 1 h / 20 °C 4.2: pH 6.0 - 7.0 View Scheme | |
Multi-step reaction with 4 steps 1.1: magnesium hydroxide / acetonitrile / 0.5 h / 10 °C 1.2: 5 h 2.1: methanol; tin(II) chloride dihdyrate / 23 h / 10 °C 3.1: magnesium hydroxide / dichloromethane; water / 0.5 h / 10 °C 3.2: 3 h 4.1: sodium tetrahydroborate; methanol / 1 h View Scheme |
2-methyl-4-nitrobenzoic acid
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: SOCl2 2: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 3: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 4: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 5: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
methyl 5-chloro-2-nitrobenzoate
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 9 steps 1.1: SnCl2*2H2O; conc. HCl / ethanol / 20 °C 2.1: 85 percent / pyridine / 20 °C 3.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 4.1: t-BuOK / toluene / 0.5 h / Heating 4.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 5.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 6.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 7.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 8.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 9.1: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
7-chloro-1,2,3,4-tetrahydro-5H-benzo[b]azepin-5-one
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 2: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 3: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 4: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: sodium hydrogencarbonate / dichloromethane; water / pH 7 - 8 2.1: tin(ll) chloride / methanol / 16 h / 20 °C 3.1: sodium hydrogencarbonate / dichloromethane / 0 - 5 °C / pH 7 - 8 4.1: sodium tetrahydroborate; methanol / 1 h / 20 °C 4.2: pH 6 - 7 View Scheme | |
Multi-step reaction with 4 steps 1.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 2.1: tin(IV) chloride / methanol / 16 h / 20 °C 3.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 4.1: sodium tetrahydroborate / methanol / 1 h / 20 °C 4.2: pH 6.0 - 7.0 View Scheme | |
Multi-step reaction with 4 steps 1: potassium carbonate; triphenylphosphine; palladium diacetate / N,N-dimethyl-formamide; water / 8 h / 120 °C / 22502.3 Torr / Autoclave 2: iron; ammonium chloride / water; methanol / 6 h / 35 - 40 °C 3: pyridine / dichloromethane / 2 h / 0 - 10 °C 4: sodium tetrahydroborate; methanol / 1 h / 15 - 30 °C View Scheme | |
Multi-step reaction with 4 steps 1.1: magnesium hydroxide / acetonitrile / 0.5 h / 10 °C 1.2: 5 h 2.1: methanol; tin(II) chloride dihdyrate / 23 h / 10 °C 3.1: magnesium hydroxide / dichloromethane; water / 0.5 h / 10 °C 3.2: 3 h 4.1: sodium tetrahydroborate; methanol / 1 h View Scheme |
N-p-toluenesulfonyl-5-chloro-anthranilic acid methyl ester
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1.1: 94 percent / K2CO3 / dimethylformamide / 4 h / 120 °C 2.1: t-BuOK / toluene / 0.5 h / Heating 2.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 3.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 4.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 5.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 6.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 7.1: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
7-chloro-1-(4-methylbenzenesulfonyl)-2,3,4,5-tetrahydro-1H-1-benzazepin-5-one
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 2: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 3: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 4: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 5: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
1-(4-amino-2-methylbenzoyl)-7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 2 steps 1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 2: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme | |
Multi-step reaction with 2 steps 1.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 2.1: sodium tetrahydroborate / methanol / 1 h / 20 °C 2.2: pH 6.0 - 7.0 View Scheme |
1-(4-nitro-2-methylbenzoyl)-7-chloro-5-oxo-2,3,4,5-tetrahydro-1H-1-benzazepine
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 3 steps 1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 2: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 3: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme | |
Multi-step reaction with 3 steps 1.1: tin(ll) chloride / methanol / 16 h / 20 °C 2.1: sodium hydrogencarbonate / dichloromethane / 0 - 5 °C / pH 7 - 8 3.1: sodium tetrahydroborate; methanol / 1 h / 20 °C 3.2: pH 6 - 7 View Scheme | |
Multi-step reaction with 3 steps 1.1: tin(IV) chloride / methanol / 16 h / 20 °C 2.1: sodium hydrogencarbonate / water; dichloromethane / 0 - 5 °C / pH 7.0 - 8.0 3.1: sodium tetrahydroborate / methanol / 1 h / 20 °C 3.2: pH 6.0 - 7.0 View Scheme |
methyl 5-chloro-2-[N-(3-ethoxycarbonyl)propyl-N-p-toluenesulfonyl]aminobenzoate
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1.1: t-BuOK / toluene / 0.5 h / Heating 1.2: 60 percent / conc. HCl / acetic acid / 5 h / Heating 2.1: 81 percent / polyphosphoric acid / 1.5 h / 80 - 100 °C 3.1: 32 percent / Et3N / CH2Cl2 / 2 h / 20 °C 4.1: 39 percent / SnCl2*2H2O; conc. HCl / ethanol / 20 °C 5.1: 53 percent / Et3N / CH2Cl2 / 1.5 h / 20 °C 6.1: 30 percent / NaBH4 / methanol / 1 h / 20 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: N-ethyl-N,N-diisopropylamine / dichloromethane / 4 h / 20 °C 2: potassium tert-butylate / toluene / 1 h / 120 °C 3: acetic acid; hydrogenchloride / water / 6 h / 100 °C 4: hydrogenchloride; tin(II) chloride dihdyrate / ethanol / 4 h / 20 °C 5: N-ethyl-N,N-diisopropylamine / dichloromethane / 2 h / 20 °C 6: sodium tetrahydroborate; methanol / 2 h / 0 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 5 steps 1: potassium tert-butylate / toluene / 1 h / 120 °C 2: acetic acid; hydrogenchloride / water / 6 h / 100 °C 3: hydrogenchloride; tin(II) chloride dihdyrate / ethanol / 4 h / 20 °C 4: N-ethyl-N,N-diisopropylamine / dichloromethane / 2 h / 20 °C 5: sodium tetrahydroborate; methanol / 2 h / 0 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: acetic acid; hydrogenchloride / water / 6 h / 100 °C 2: hydrogenchloride; tin(II) chloride dihdyrate / ethanol / 4 h / 20 °C 3: N-ethyl-N,N-diisopropylamine / dichloromethane / 2 h / 20 °C 4: sodium tetrahydroborate; methanol / 2 h / 0 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 4 steps 1: dichloromethane / 4.5 h / 20 °C / Reflux 2: hydrogenchloride; tin(II) chloride dihdyrate / water; ethanol / 3 h / 20 °C 3: triethylamine / dichloromethane / 2.25 h / 20 °C 4: sodium tetrahydroborate; methanol / 5 h / 20 °C View Scheme |
4-chloro-aniline
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 8 steps 1: sodium carbonate / acetonitrile / 4 h / 80 °C 2: triethylamine / dichloromethane / 3 h / 20 °C 3: sodium hydroxide / 1.5 h / 50 °C 4: thionyl chloride / dichloromethane / 2 h / 20 °C / Reflux 5: dichloromethane / 4.5 h / 20 °C / Reflux 6: hydrogenchloride; tin(II) chloride dihdyrate / water; ethanol / 3 h / 20 °C 7: triethylamine / dichloromethane / 2.25 h / 20 °C 8: sodium tetrahydroborate; methanol / 5 h / 20 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 7 steps 1: triethylamine / dichloromethane / 3 h / 20 °C 2: sodium hydroxide / 1.5 h / 50 °C 3: thionyl chloride / dichloromethane / 2 h / 20 °C / Reflux 4: dichloromethane / 4.5 h / 20 °C / Reflux 5: hydrogenchloride; tin(II) chloride dihdyrate / water; ethanol / 3 h / 20 °C 6: triethylamine / dichloromethane / 2.25 h / 20 °C 7: sodium tetrahydroborate; methanol / 5 h / 20 °C View Scheme |
tolvaptan
Conditions | Yield |
---|---|
Multi-step reaction with 6 steps 1: sodium hydroxide / 1.5 h / 50 °C 2: thionyl chloride / dichloromethane / 2 h / 20 °C / Reflux 3: dichloromethane / 4.5 h / 20 °C / Reflux 4: hydrogenchloride; tin(II) chloride dihdyrate / water; ethanol / 3 h / 20 °C 5: triethylamine / dichloromethane / 2.25 h / 20 °C 6: sodium tetrahydroborate; methanol / 5 h / 20 °C View Scheme |
Conditions | Yield |
---|---|
Stage #1: Dibenzyl N,N-diisopropylphosphoramidite; tolvaptan With 1H-tetrazole In dichloromethane at 20℃; for 2h; Stage #2: With 3-chloro-benzenecarboperoxoic acid In dichloromethane at -40 - 0℃; for 1h; | 97.2% |
Multi-step reaction with 2 steps 1: 2H-tetrazole / dichloromethane / 2 h / 20 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 1 h / -40 - 0 °C View Scheme |
tolvaptan
C26H26ClN2O6P
Conditions | Yield |
---|---|
Stage #1: tolvaptan With triethylamine; trichlorophosphate In 1,2-dimethoxyethane at -15 - -12℃; for 2h; Stage #2: With sodium hydroxide; water In 1,2-dimethoxyethane; toluene at 0 - 50℃; Stage #3: With hydrogenchloride; water at 10℃; Product distribution / selectivity; | 97% |
Multi-step reaction with 3 steps 1: 2H-tetrazole / dichloromethane / 2 h / 20 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 1 h / -40 - 0 °C 3: 5%-palladium/activated carbon; hydrogen / ethanol / 0.17 h View Scheme | |
Multi-step reaction with 2 steps 1.1: 1H-tetrazole / dichloromethane / 2 h / 20 °C 1.2: 1 h / -40 - 0 °C 2.1: 5%-palladium/activated carbon; hydrogen / ethanol View Scheme |
Conditions | Yield |
---|---|
Stage #1: tolvaptan With pyridine; diphenyl hydrogen phosphite at 0 - 20℃; for 0.5h; Stage #2: methanol at 20℃; for 0.5h; | 91% |
tolvaptan
Conditions | Yield |
---|---|
With 1,3-bis(2,6-diisopropylphenyl)-2-fluoroimidazolium tetrafluoroborate; cesium fluoride In toluene at 80℃; for 17h; Inert atmosphere; Schlenk technique; Sealed tube; | 86% |
tolvaptan
Conditions | Yield |
---|---|
Stage #1: tolvaptan With triethylamine; trichlorophosphate In 1,2-dimethoxyethane at -18 - -13℃; for 2h; Inert atmosphere; Large scale; Stage #2: With water; sodium hydroxide In 1,2-dimethoxyethane at -3 - 30℃; for 0.5h; Inert atmosphere; Large scale; | 86% |
Multi-step reaction with 4 steps 1: 2H-tetrazole / dichloromethane / 2 h / 20 °C 2: 3-chloro-benzenecarboperoxoic acid / dichloromethane / 1 h / -40 - 0 °C 3: 5%-palladium/activated carbon; hydrogen / ethanol / 0.17 h 4: sodium hydroxide / methanol; water / 0.08 h / Cooling with ice View Scheme | |
Multi-step reaction with 3 steps 1.1: 1H-tetrazole / dichloromethane / 2 h / 20 °C 1.2: 1 h / -40 - 0 °C 2.1: 5%-palladium/activated carbon; hydrogen / ethanol 3.1: sodium hydroxide / methanol; water / 0.08 h / Cooling with ice View Scheme |
Conditions | Yield |
---|---|
Stage #1: tolvaptan With pyridine; diphenyl hydrogen phosphite at 20℃; for 0.5h; Stage #2: 3-Hydroxypropionitrile at 20℃; for 0.5h; | 75% |
tolvaptan
n-hexadecanoyl chloride
{7-chloro-1-[2-methyl-4-(2-methyl-benzoylamino)-benzoyl]-2,3,4,5-tetrahydro-1H-benzo[b]azepin-5-yl} hexadecanoate
Conditions | Yield |
---|---|
With pyridine In dichloromethane at 20℃; | 74% |
tolvaptan
Conditions | Yield |
---|---|
Stage #1: tolvaptan With triethylamine; phosphorus trichloride In tetrahydrofuran at -10℃; for 2h; Stage #2: With sodium hydroxide; water In tetrahydrofuran at 0℃; Product distribution / selectivity; | 60% |
Stage #1: tolvaptan With pyridine; diphenyl hydrogen phosphite at 20℃; for 1h; Stage #2: With water at 20℃; for 0.5h; Product distribution / selectivity; | 24% |
Conditions | Yield |
---|---|
Stage #1: tolvaptan With pyridine; diphenyl hydrogen phosphite at 0 - 20℃; for 1h; Stage #2: ethanol at 20℃; for 0.5h; | 38% |
Conditions | Yield |
---|---|
Stage #1: tolvaptan With triethylamine; trichlorophosphate In tetrahydrofuran for 0.5h; Cooling with ice/methanol; Stage #2: methanol With triethylamine In tetrahydrofuran for 0.5h; | 33% |
Conditions | Yield |
---|---|
Stage #1: tolvaptan With pyridine; diphenyl hydrogen phosphite at 20℃; for 1h; Stage #2: glycolic acid methyl ester at 20℃; for 12h; | 20% |
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