Teva Pharmaceutical Industries Limited

Yaron Shmuely

Santiago Ini

Ben-Zion Dolitzky

Evgeny Shapiro

Kobi Chen

Mili Abramov

Eli Lancry

Naama Chasid

The present invention relates to a process for preparing paliperidone from its intermediate 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one.

Process for the synthesis of 9-hydroxy risperidone (paliperidone)

The present invention provides 3-benzyloxy-2-aminopyridine (BOPA), 3-(2-Hydroxyethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (HMBP), 3-(2-Chloroethyl)-2-methyl-9-hydoxy-4H-pyrido[1,2-a]pyrimidine-4-one (CMHP) and 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrrido[1,2-a]-pyrimidin-4-one (CMHTP) useful as intermediates for the preparation of paliperidone. The present invention also provides processes for preparing these intermediates and for preparing paliperidone.

Process for the synthesis of CMHTP and intermediates thereof

A chiral resolution process for the preparation of (S)-AT-OL, and a process for the racemization of AT-OL are provided.

Process for the preparation of (S)-(-)-N,N-dimethyl-3-(2-thienyl)-3-hydroxypropananine, a duloxetine intermediate

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Hedera, Israel

Yaron Shmuely