Piramal Pharma Limited

Rajesh Shenoy

Sharadsrikar Kotturi

Rajender Reddy Leleti

Chirag Patel

Yogesh Waman

Aditya Patwa

The present invention relates to an improved asymmetric synthesis of alpha-(diarylmethyl) alkyl amines (hereafter referred to as the compound (1)) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective lithiation of alpha-diarylmethanes. followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of chiral alpha-(diarylmethyl) alkyl amines 4 and chiral amine 5; which on subsequently removing the sulfinyl group provides corresponding alpha-(diarylmethyl) alkyl amines (1) or relative chiral amines (1&#x2033;).

Asymmetric synthesis of alpha-(diarylmethyl) alkyl amines

The present invention relates to an improved asymmetric synthesis of alpha-branched amines (hereafter referred to as the compound) and relative chiral amines (1&#x2033;) or its pharmaceutically acceptable salt and derivatives. The process comprises an unusual substrate specific regioselective ortho lithiation of substituted arene compounds, followed by its highly diastereoselective addition to N-tert-butanesulfinylimines resulting in the selective formation of alpha-branched sulfinyl amine and chiral amine; which on subsequently removing the sulfinyl group provides corresponding alpha-branched amines or relative chiral amines (1&#x2033;).

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Gujarat, India

Rajesh Shenoy