250214-39-2

Upstream product

• 837376-33-7 4-(benzyloxy)-3-(3-(diisopropylamino)-1-phenylpropyl)benzaldehyde 
• 286930-05-0 (+)-N,N-Diisopropyl-3-(2-benzyloxy-5-carbomethoxyphenyl)-3-phenylpropylamine 
• 701906-29-8 (+)-N,N-Diisopropyl-3-(2-benzyloxy-5-carboxyphenyl)-3-phenylpropylamine 
• 1349883-68-6 (+/-)-4-bromo-2-(3-hydroxy-1-phenylpropyl)phenol 
• 250214-37-0 (+/-)-toluene-4-sulphonic acid 3-(2-benzyloxy-5-bromophenyl)-3-phenylpropyl ester 
• 156755-23-6 6-bromo-4-phenyl-3,4-dihydro-2H-chromen-2-one 

Downstream Products

• 207679-81-0 (R)-2-[3-(diisopropylamino)-1-phenylpropyl]-4-(hydroxymethyl)-phenol 
• 286930-02-7 fesoterodine 
• 1350462-15-5 lithium (R)-(+)-2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethylphenol 
• 286930-03-8 fesoterodine fumarate 
• 200801-70-3 RS-N,N-diisopropyl-3-(2-hydroxy-5-(hydroxymethyl)phenyl)-3-phenylpropylamine 

Relevant academic research and scientific papers

PROCESS FOR PREPARATION OF PHENOLIC MONOESTERS OF HYDROXYMETHYL PHENOLS

Disclosed herein is an improved and efficient process for preparation of fesoterodine and its pharmaceutically acceptable salt. Disclosed also herein is novel intermediate of formula (III). Also disclosed are metal salts of formula (XII) and preparation thereof.

PROCESS FOR PREPARATION OF PHENOLIC MONOESTERS OF HYDROXYMETHYL PHENOLS

A process for the preparation of phenolic monoesters of 2-(3-diisopropylamino-1-phenylpropyl)-4-(hydroxymethyl)phenol by converting (±)6-halo-4-phenylchroman-2-one to (±)4-halo-2-(3-hydroxy-1-phenylpropyl)phenol. The two hydroxyl groups are protected and the protected compound is reacted with diisopropylamine to give (±)[3-(2-benzyloxy-5-halophenyl)-3-phenylpropyl]diisopropylamine. The halo substituent on the benzene ring is converted to corresponding benzyl alcohol and then the protection is removed to give racemic 5-HMT. Racemic 5-HMT is converted R enantiomer and then it is esterified.

Fesoterodine Substantially Free of Dehydroxy Impurity

Provided herein is an impurity of fesoterodine, fesoterodine dehydroxy impurity, 2-[(1R)-3-[bis(1-methylethy)amino]-1-phenylpropyl]-4-methylphenyl isobutyrate, and a process for preparing and isolating thereof. Provided further herein is a highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of fesoterodine dehydroxy impurity, process for the preparation thereof, and pharmaceutical compositions comprising highly pure fesoterodine or a pharmaceutically acceptable salt thereof substantially free of dehydroxy impurity. Provided also herein is a pharmaceutical composition comprising solid particles of pure fesoterodine fumarate substantially free of dehydroxy impurity, wherein 90 volume-percent of the particles (D90) have a size of less than about 200 microns.

PROCESS FOR PREPARATION OF 2-(3-DIISOPROPYLAMINO-1-PHENYLPROPYL)-4-HYDROXYMETHYL-PHENOL, A METABOLITE OF TOLTERODINE

The present invention relates to processes for preparation of 2-(3-diisopropylamino-1-phenylpropyl)-4-hydroxymethyl-phenol of Formula I, which is a metabolite of tolterodine.

3,3-Diphenylpropylamines, their use and preparation

The invention relates to 3,3-diphenylpropylamines of formula (I), wherein R1 signifies hydrogen or methyl, R2 and R3 independently signify hydrogen, methyl, methoxy, hydroxy, carbamoyl, sulphamoyl or halogen, and X represents a tertiary amino group of for