Intermediates for the production of (+) biotin

C - Chemistry – Metallurgy – 07 – D

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260/298.3

C07D 491/048 (2006.01) C07F 7/10 (2006.01) C07F 9/547 (2006.01)

Patent

CA 1329936

Intermediates FOR THE PRODUCTION OF (+) BIOTIN ABSTRACT Process for the production of (+) biotin. The process comprises catalytically hydrogenating a compound of the formula: Image I with hydrogen, separating the desired diastereomer of the formula: Image II introducing a protective group, converting the diastereomer by further reaction with a thiocarboxylic acid salt derivative into the corresponding thiolactone by a Grignard reaction and subsequently splitting off of water or a compound of the formula: (C6H5)3p?(CH2)4COOR3.X? III 58 in the presence of a base to a compound of the formula: Image IV catalytically hydrogenating the compound and then cleaving the protective groups to form (+) biotin. The process starts from a readily-available intermediate product and employs relatively few industrially-feasible step. 59

616416

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