Sun Pharmaceutical Industries Limited

Ajay Sohanlal Midha

Rajamannar Thennati

Trinadha Rao Chitturi

Hemant Ashvinbhai Chokshi

Keshav Deo

Tilak Chandra

Vijay Muljihhai Patel

A compound of formula I wherein X, Y, X' & Y&#x2032; are selected from hydrogen, halogen, substituted or unsubstituted alkyl (linear, branched or cyclo), aryl, alkyloxy and haloalkyl group; R, R, R& Rare selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; wherein the substituents R& Ron the piperazinyl moiety are either syn or anti to each other and optionally Rand Rtogether with the carbons to which they are attached form a monocyclic saturated or aryl or substituted aryl or heteroaryl or substituted heteroaryl ring containing one or more hetero atoms selected from N, S and O with a ring size ranging from 3 to 6; with a proviso that when R& Rtogether do not form part of a ring they may exist in either E or Z configuration; Ris (CH)&#x2014;O&#x2014;CH&#x2014;CO-Z wherein n is 1 to 6; Z is selected from OH, OR, NRR&#x2032;, N(OR)R&#x2032;, N(R)&#x2014;N(R)R&#x2032;and wherein R & R&#x2032; are selected from hydrogen, substituted or unsubstituted alkyl groups (linear, branched or cyclo), aryl, heteroaryl groups or aralkyl groups, heterocycles containing one or more of hetero atoms (viz., N, S, O), substituted or unsubstituted alkenyl or alkynyl groups of carbon 2 to 6; and B is selected from &#x2014;(CH)n-(n is 1 to 6) and &#x2014;(CH)x-D-(CH)y where D is O, NR, S or SO, x and y are independently 1 to 6; and m is selected from 1 to 6; and pharmaceutically acceptable salts thereof.

4-(diarylmethyl)-1-piperazinyl derivatives

A new process is described for the preparation of (alkoxyalkyl)(4-trifluoromethylphenyl)methanones. The process comprises reacting a 4-trifluoromethylbenzonitrile with an alkoxyalkyl Grignard in the presence of a suitable polar aprotic solvent. The compound (4-methoxybutyl)(4-trifluoromethylphenyl)methanone is useful as an intermediate in the preparation of the antidepressant drug fluvoxamine.

Process for the synthesis of alkoxyalkyl (trifluormethylphenyl) methanones

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Baroda, India

Ajay Sohanlal Midha