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

Abstract: The present invention relates to a method of preparing racemic nicotine comprising: (i) reacting ethyl nicotinate and N-vinylpyrrolidone in the presence of an alcoholate base to 3-nicotinoyl-1-vinylpyrrolidin-2-one; (ii) reacting the 3-nicotinoyl-1-vinylpyrrolidin-2-one with an acid to myosmine; (iii) reducing the myosmine to nornicotine using a reducing agent; and (iv) methylating the nornicotine to obtain the racemic nicotine.

Abstract: The present invention relates to a method of separating racemic nicotine of Formula (1-a) as a mixture of the (R)- and (S)-enantiomers into the enantiomerically pure (S)- and (R)-nicotine represented by Formula (1-b) and (1-c), by adding a mixture of the L- and the D-enantiomer of a O,O?-disubstituted tartaric acid, wherein the molar ratio of the L- to the D-enantiomer is from 80:20 to 95:5, and obtaining the (S)-nicotine of formula (1-b), or by adding O,O?-dibenzoyl-D-tartaric acid and obtaining the (R)-nicotine of formula (1-c).

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

Abstract: 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.

Abstract: The present invention relates to a method of preparing racemic nicotine comprising: (i) reacting ethyl nicotinate and N-vinylpyrrolidone in the presence of an alcoholate base to 3-nicotinoyl-1-vinylpyrrolidin-2-one; (ii) reacting the 3-nicotinoyl-1-vinylpyrrolidin-2-one with an acid to myosmine; (iii) reducing the myosmine to nornicotine using a reducing agent; and (iv) methylating the nornicotine to obtain the racemic nicotine.

Abstract: 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.

Abstract: The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.

Abstract: The present invention relates to the improved synthesis of noroxymorphone of formula (III). Particularly, the invention shows a way how to reduce the impurity level in the product avoiding lengthy purification steps.

Abstract: The current invention offers a process for the production of N-Boc-2-amino-3,3-dimethylbutyric acid by a reaction of tert-Leucine with di-tert-butyl-dicarbonate, the process comprising (i) contacting the tert-Leucine with di-tert-butyl-dicarbonate in an aqueous medium, optionally comprising a first organic solvent, in the presence of an inorganic base, (ii) optionally removing the first organic solvent, (iii) optionally extracting the resulting N-Boc-2-amino-3,3-dimethylbutyric acid into a second organic solvent, (iv) isolating the product by precipitation from the reaction mixture at acidic pH, and (v) optionally reuse the first and/or second organic solvents recovered from step (ii) and/or step (iv) for the next production cycle. The process is sufficiently short, uses preferably environmental friendly solvents, avoids waste and leads to good yields.

Abstract: The present invention relates to a method of separating racemic nicotine of Formula (1-a) as a mixture of the (R)- and (S)-enantiomers into the enantiomerically pure (S)- and (R)-nicotine represented by Formula (1-b) and (1-c), by adding a mixture of the L- and the D-enantiomer of a O,O?-disubstituted tartaric acid, wherein the molar ratio of the L- to the D-enantiomer is from 80:20 to 95:5, and obtaining the (S)-nicotine of formula (1-b), or by adding O,O?-dibenzoyl-D-tartaric acid and obtaining the (R)-nicotine of formula (1-c).

Abstract: The present invention relates to a method of preparing racemic nicotine comprising: (i) reacting ethyl nicotinate and N-vinylpyrrolidone in the presence of an alcoholate base to 3-nicotinoyl-1-vinylpyrrolidin-2-one; (ii) reacting the 3-nicotinoyl-1-vinylpyrrolidin-2-one with an acid to myosmine; (iii) reducing the myosmine to nornicotine using a reducing agent; and (iv) methylating the nornicotine to obtain the racemic nicotine.

Abstract: The current invention offers a process for the production of N-Boc-2-amino-3,3-dimethylbutyric acid by a reaction of tert-Leucine with di-tert-butyl-dicarbonate, the process comprising (i) contacting the tert-Leucine with di-tert-butyl-dicarbonate in an aqueous medium, optionally comprising a first organic solvent, in the presence of an inorganic base, (ii) optionally removing the first organic solvent, (iii) optionally extracting the resulting N-Boc-2-amino-3,3-dimethylbutyric acid into a second organic solvent, (iv) isolating the product by precipitation from the reaction mixture at acidic pH, and (v) optionally reuse the first and/or second organic solvents recovered from step (ii) and/or step (iv) for the next production cycle. The process is sufficiently short, uses preferably environmental friendly solvents, avoids waste and leads to good yields.

Abstract: The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogs of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.

Abstract: The present invention relates to a method of preparing a compound of Formula II-a? or Formula II-b?, wherein RI represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RII represents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RIII represents 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; RIV represents 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 RV represents hydrogen or a methyl group; wherein RI and RII are different from each other.

Abstract: The present invention relates to a method of preparing a compound of Formula II-a? or Formula II-b?, wherein RI represents hydrogen or a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RII represents a linear, branched and/or cyclic alkyl or alkenyl group having 1 to 10 carbon atoms; RIII represents 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; RIV represents 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 RV represents hydrogen or a methyl group; wherein RI and RII are different from each other.

Abstract: The invention relates to an improved method of preparing buprenorphine, a salt thereof, analogues of buprenorphine and their salts. In particular, the invention relates to a method of preparing buprenorphine and related products and salts in economic and ecologic ways having increased yields.

Abstract: The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages.

Abstract: The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages.

Abstract: The present invention provides an efficient method of making O-desmethyl-venlafaxine.