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1. (WO2012046254) PROCESS FOR PREPARING AN INTERMEDIATE OF SITAGLIPTIN VIA ENZYMATIC CONVERSION
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2012/046254    International Application No.:    PCT/IN2011/000702
Publication Date: 12.04.2012 International Filing Date: 10.10.2011
Chapter 2 Demand Filed:    26.04.2012    
IPC:
C07D 487/04 (2006.01), C12N 9/02 (2006.01), C12P 17/18 (2006.01)
Applicants: CADILA HEALTHCARE LIMITED [IN/IN]; Zydus Tower Satellite Cross Road Ahmedabad 380015 Gujarat (IN) (For All Designated States Except US).
MENDIRATTA, Sanjeev Kumar [IN/IN]; (IN) (For US Only).
PANDEY, Bipin [IN/IN]; (IN) (For US Only).
JOSHI, Rupal [IN/IN]; (IN) (For US Only).
TRIVEDI, Umang [IN/IN]; (IN) (For US Only).
DAVE, Mayank, G. [IN/IN]; (IN) (For US Only).
KOTHARI, Himanshu, M. [IN/IN]; (IN) (For US Only).
SHUKLA, Bhavin [IN/IN]; (IN) (For US Only)
Inventors: MENDIRATTA, Sanjeev Kumar; (IN).
PANDEY, Bipin; (IN).
JOSHI, Rupal; (IN).
TRIVEDI, Umang; (IN).
DAVE, Mayank, G.; (IN).
KOTHARI, Himanshu, M.; (IN).
SHUKLA, Bhavin; (IN)
Agent: SUBRAMANIAM, Hariharan; Subramaniam, Nataraj & Associates E- 556, Greater Kailash-II New Delhi 110048 (IN)
Priority Data:
2805/MUM/2010 08.10.2010 IN
Title (EN) PROCESS FOR PREPARING AN INTERMEDIATE OF SITAGLIPTIN VIA ENZYMATIC CONVERSION
(FR) MÉTHODE DE PRÉPARATION D'UN INTERMÉDIAIRE DE SITAGLIPTINE PAR CONVERSION ENZYMATIQUE
Abstract: front page image
(EN)The invention provides a process for preparing 3 -hydroxy-1-(3- (trifluoromethyl)-5,6-dihydro-[l,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl) butan-1-one (Formula I), into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms comprising: a) reacting 4-oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1- (2,4,5-trifluorophenyl)butan-2-one of formula (III) with a suitable oxidoreductase enzymes or its suitable variants in the presence of suitable conditions and co-factor b) isolating 3-hydroxy-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin- 7(8H)-yl)-4-(2,4,5-trifluorophenyl) butan-1-one, into its racemic (R/S) form or any of its optically active (S) or (R) forms or enantiomeric excess mixture of any of the forms
(FR)L'invention concerne une méthode de préparation de 3-hydroxy-1-(3-(trifluorométhyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophényl)butane-1-one (formule I), pour obtenir la forme racémique (R/S) ou l'une quelconque des formes (S) ou (R) optiquement actives du composé, ou le mélange d'énantiomères excédentaires de l'une quelconque desdites formes. La méthode consiste à: a) mettre en réaction 4-oxo-4-[3-(trifluorométhyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl]-1-(2,4,5-trifluorophényl)butane-2-one de formule (III) avec une enzyme d'oxydoréductase appropriée ou les variants appropriés de celle-ci, dans des conditions appropriées et en présence d'un co-facteur approprié; b) isoler 3-hydroxy-1-(3-(trifluorométhyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophényl)butane-1-one, pour obtenir la forme racémique (R/S) ou l'une quelconque des formes (S) ou (R) optiquement actives du composé, ou le mélange d'énantiomères excédentaires de l'une quelconque desdites formes.
Designated States: AE, AG, AL, AM, AO, AT, AU, AZ, BA, BB, BG, BH, BR, BW, BY, BZ, CA, CH, CL, CN, CO, CR, CU, CZ, DE, DK, DM, DO, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, GT, HN, HR, HU, ID, IL, IN, IS, JP, KE, KG, KM, KN, KP, KR, KZ, LA, LC, LK, LR, LS, LT, LU, LY, MA, MD, ME, MG, MK, MN, MW, MX, MY, MZ, NA, NG, NI, NO, NZ, OM, PE, PG, PH, PL, PT, QA, RO, RS, RU, RW, SC, SD, SE, SG, SK, SL, SM, ST, SV, SY, TH, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LR, LS, MW, MZ, NA, RW, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AL, AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HR, HU, IE, IS, IT, LT, LU, LV, MC, MK, MT, NL, NO, PL, PT, RO, RS, SE, SI, SK, SM, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: English (EN)
Filing Language: English (EN)