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Siegfried Aktiengesellschaft

Stefan Sahli

Beat Theodor Weber

Frank Himmelsbach

Matthias Eckhardt

Xiao-Jun Wang

Bing-Shiou Yang

Chutian Shu

Monika Brink

Beat Weber

Intermediate compounds are described herein and which are used to manufacture a crystalline compound 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#x3b2;-D-glucopyranos-1-yl)-benzene L-proline monohydrate.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#xdf;-d-glucopyranos-1-yl)-benzene, L-proline and water

The invention relates to a process for the manufacture of the crystalline compound according to formula (I) comprising the steps (a) deacetylating the final intermediate (FI), (b) forming the crystalline compound according to formula (I) by reacting the deacetylated final intermediate of step (a) with L-proline and water and isolating the final reaction product; processes of manufacturing intermediates thereof; process intermediates and their uses in the processes according to the present invention.

Synthesis of 1:1:1 co-crystal of 1-cyano-2-(4-cyclopropyl-benzyl)-4-(&#x3b2;-D-glucopyranos-1-yl)-benzene, L-proline and water

The present invention relates to a method of preparing a compound of Formula II-a' or Formula II-b&#x2032;, wherein Rrepresents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; Rrepresents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; Rrepresents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms or a linear, branched and/or cyclic alkoxy group having 1 to 10 carbon atoms; Rrepresents hydrogen or a linear, branched and/or cyclic alkyl group having 1 to 10 carbon atoms or an optionally substituted aryl or alkylaryl group having 6 to 40 carbon atom or acetyl or silyl or a protective group; and Rrepresents hydrogen or a methyl group; wherein Rand Rare different from each other. 

Method of manufacturing stereoisomers of buprenorphine and analogues thereof

The present invention relates to a novel process for preparing opiates or salts thereof. More particularly, the present invention relates to oxidizing the starting material in a continuous flow reactor, followed by either an isolation of the intermediate, or a direct reduction reaction.

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Zofingen, Switzerland

Stefan Sahli