Sun Pharmaceutical Industries Limited

Kanaksinh Jesingbhai Jadav

Rajamannar Thennati

Trinadha Rao Chitturi

Hemant Ashvinbhai Shah

Shivramchandra Kanangi

Kamleshkumar Naranbhai Borkhataria

Raja Sekhar Unnam

Rutvij Manharlal Bhatt

Sudhakar Kambhampati

The present invention provides a process for preparing a compound of formula (I), or a pharmaceutically acceptable salt thereof, having the R-configuration, of formula (IA), or S-configuration of formula (IB), selectively over the other enantiomer. 

Process for the preparation of chiral beta amino carboxamide derivatives

The present invention provides substantially pure desloratadine having an HPLC purity greater than 99.5% and having an absorbance less than 0.15 Au at 420 nm for a 5% w/v solution in methanol, which does not show a peak for an impurity at a relative retention time in the range from about 0.85 to about 0.99 (relative to desloratadine appearing at a retention time of 25&#xb1;5 minutes), which is greater than the discard limit set at less than 0.025% of the total area, when tested according to an HPLC method performed using a Hypersil BDS Ccolumn (15 cm&#xd7;4.6 mm, 5 &#x3bc;m particle size) with the following parameters:  The present invention also provides a process for the preparation of substantially pure desloratadine by the process comprising acidic hydrolysis of a compound of formula 3 where R is selected from COR, COORwherein Ris selected from branched or linear alkyl (1-6 C), cycloalkyl, alkenyl, alkynyl, aryl, aralkyl and their substituted analogs; and their substituted analogs with a strong organic acid or a mineral acid. 

Process of preparing desaloratadine

The present invention provides a convenient process for the preparation of S-fluoromethyl 6&#x3b1;,9&#x3b1;-difluoro-11&#x3b2;-hydroxy-16&#x3b1;-methyl-17&#x3b1;-propionyloxy-3-oxoandrosta-1,4-diene-17&#x3b2;-carbothioate, a compound of formula 1, comprising

Synthesis of s-fluoromethyl 6&#x3b1;,9&#x3b1;-difluoro-11&#x3b2;-hydroxy-16&#x3b1;-methyl-17&#x3b1;-propionyloxy-3-oxoandrosta-1,4-diene-17&#x3b2;-carbothioate

A process for converting the cis (1R, 4R), trans (1S, 4R), and trans (1R, 4S) stereoisomers of sertraline into sertraline comprises, starting with an initial reaction mixture which contains at least one of these stereoisomers, converting the sertraline stereoisomers into an imine form of sertraline. The imine form of sertraline is then reduced so that sertraline and at least one sertraline stereoisomer byproduct is produced in the reaction mixture. The sertraline is then recovered from the reaction mixture, e.g., by fractional crystallization (followed by resolution of sertraline from the cis (1R, 4R) stereoisomer, if necessary). The reaction mixture is then recycled through the same steps so that sertraline is produced from its stereoisomers in an asymptotic yield.

Process for converting stereoisomers of sertraline into sertraline

A process is described for the preparation of substantially pure fluvoxamine maleate, an important antidepressant drug of the formula I, for use as an active pharmaceutical ingredient (API), from the corresponding oxime viz 5-methoxy-4&prime;-trifluoromethylvalerophenone oxime of formula II.

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Baroda, India

Kanaksinh Jesingbhai Jadav