740780-79-4

Basic information

• Product Name: (1R,3R)-Solifenacin Succinate 2
• Synonyms: (1R,3R)-Solifenacin Succinate 2
• CAS NO: 740780-79-4
• Molecular Formula: C₂₃H₂₆N₂O₂
• Molecular Weight: 362.46474
• Mol File: 740780-79-4.mol
• Article Data: 9

Chemical Properties

• Boiling Point: 505.5±50.0 °C(Predicted)
• Appearance: /
• Density: 1.24±0.1 g/cm3(Predicted)
• PKA: 9.03±0.33(Predicted)
• CAS DataBase Reference: (1R,3R)-Solifenacin Succinate 2(CAS DataBase Reference)
• NIST Chemistry Reference: (1R,3R)-Solifenacin Succinate 2(740780-79-4)
• EPA Substance Registry System: (1R,3R)-Solifenacin Succinate 2(740780-79-4)

Safety Data

• Hazardous Substances Data: 740780-79-4(Hazardous Substances Data)

Usage

Description

(1R,3R)-Solifenacin Succinate 2 is a quinuclidine-based chemical compound that functions as a medication for treating overactive bladder. It operates by inducing relaxation in the bladder muscles, which in turn diminishes the frequency of the urge to urinate. (1R,3R)-Solifenacin Succinate 2 is orally administered in tablet form, ensuring efficient absorption into the bloodstream. It undergoes metabolism in the liver and is excreted through urine, exhibiting a half-life of approximately 65 hours. While it may cause side effects such as dry mouth, constipation, and occasional difficulty urinating, these are generally mild and well-tolerated by patients.

Uses

Used in Pharmaceutical Industry:
(1R,3R)-Solifenacin Succinate 2 is utilized as a therapeutic agent for the management of overactive bladder conditions. It is particularly effective due to its ability to relax the bladder muscles, leading to a significant reduction in the frequency of urination. This application is crucial for improving the quality of life for patients suffering from such conditions, providing them with a more manageable and comfortable daily routine.

Upstream product

• 180272-14-4 (S,R)-((R)-quinuclidin-3-yl) 1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 552831-23-9 (R)-imidazole-1-carboxylic acid 1-azabicyclo[2.2.2]oct-3-yl ester 
• 6970-83-8 ethyl-N-(2-phenethyl)carbamate 
• 102422-37-7 N-(1H-imidazol-1-ylcarbonyl)-2-phenethylamine 
• 25333-42-0 (R)-quinuclidin-3-ol 
• 64-04-0 phenethylamine 
• 22990-19-8 1-phenyl-1,2,3,4-tetrahydroisoquinoline 
• 1619-34-7 3-quinuclidinol 
• 180272-45-1 (R)-(-)-1-phenyl-1,2,3,4-tetrahydroisoquinoline 
• 180468-41-1 ethyl (R)-1-phenyl-3,4-dihydroisoquinoline-2(1H)-carboxylate 
• 180468-42-2 (S)-N-carboxylic acid ethyl ester-1-phenyl-1,2,3,4-tetrahydroisoquinoline 
• 3278-14-6 N-phenethylbenzamide 
• 52250-50-7 1-phenyl-3,4-dihydroisoquinoline 

Downstream Products

• 1035547-81-9 (3R)-1-azabicyclo[2.2.2]oct-3-yl (1S)-3,4-dihydro-1-phenyl-2(1H)-isoquinoline carboxylate hydrogen L-tartrate 
• 862207-71-4 (1S)-3,4-dihydro-1-phenyl-2-(1H)-isoquinolinecarboxylic acid (3S)-1-azabicyclo[2.2.2]oct-3-yl ester succinate 
• 862207-70-3 (3R)-1-azabicyclo[2.2.2]oct-3-yl (1R)-3,4-dihydro-1-phenyl-2(1H)-isoquinoline carboxylate succinate 
• 1262506-09-1 solifenacin succinate 
• 865813-73-6 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate benzenesulfonate 
• 865862-30-2 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate hydrobromide 
• 865813-83-8 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (+)-(2S,3S)-di-O-benzoyltartrate 
• 865813-76-9 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate sebacate 
• 865813-77-0 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (+)-camphor-10-sulfonate 
• 865813-84-9 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (+)-(2S,3S)-di-O-(4-methylbenzoyl)tartrate 
• 865813-79-2 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate ethanesulfonate 
• 865813-74-7 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate cyclohexanesulfamate 
• 865813-80-5 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate methanesulfonate 
• 865813-72-5 (-)-(3R)-quinuclidin-3-yl (1R)-1-phenyl-1,2,3,4-tetrahydroisoquinoline-2-carboxylate (-)-L-phenylalaninate 

Relevant articles and documents

PROCESS FOR THE PREPARATION OF SOLIFENACIN AND SALTS THEREOF

The invention provides a new process for the preparation of solifenacin or a pharmaceutically acceptable acid addition salt thereof, comprising reacting (R)- quinuclidin-3-yl phenethylcarbamate with benzaldehyde in the presence of an acid to obtain a diasteroisomeric mixture (S,R)-((R)-quinuclidin-3-yl) 1 -phenyl-3,4- dihydroisoquinoline-2(1 H)-carboxylate of formula (IV) which can be resolved and the solifenacin or a pharmaceutically acceptable acid addition salt thereof recovered. The invention also provides the new key intermediate (R)-quinuclidin-3-yl phenethylcarbamate involved in the process. Further the invention provides a method for the transformation of (R)-((R)-quinuclidin-3-yl) 1 -phenyl-3,4- dihydroisoquinoline-2(1 H)-carboxylate into a diasteroisomeric mixture (S,R)-((R)- quinuclidin-3-yl) 1 -phenyl-3,4-dihydroisoquinoline-2(1 H)-carboxylate.

PROCESS FOR PREPARING CHEMICALLY AND CHIRALLY PURE SOLIFENACIN BASE AND ITS SALTS

The present invention provides improved processes for preparing chemically and chirally pure Solifenacin base. The present invention also provides for a composition comprising of a salt of Solifenacin having at least 98 % purity. The present invention also disclose certain new salts of Solifenacin as well as well as new polymorphic forms of Solifenacin hydrochloride and Solifenacin oxalate, in pure form.

A METHOD FOR THE PREPARATION OF SOLIFENACIN

A method of preparing (lS)-(3R)-l-azabicyclo[2.2.2]oct-3-yl 3,4-dihydro-l-phenyl-2(lH)- isoquinoline carboxylate (solifenacin) or its pharmaceutically acceptable salts with high optic purity, wherein the crude solifenacin base is transformed to the hydrogen tartrate, which is then optionally transformed to another pharmaceutically acceptable salt or the base of solifenacin. A crystalline salt of solifenacin hydrogen tartrate.