WIPO logo
Mobile | Deutsch | Español | Français | 日本語 | 한국어 | Português | Русский | 中文 | العربية |
PATENTSCOPE

Search International and National Patent Collections
World Intellectual Property Organization
Search
 
Browse
 
Translate
 
Options
 
News
 
Login
 
Help
 
Machine translation
1. (WO2005016880) PROCESS FOR PRODUCTION OF cis-4-FLUORO-L-PROLINE DERIVATIVES
Latest bibliographic data on file with the International Bureau   

Pub. No.:    WO/2005/016880    International Application No.:    PCT/JP2004/011827
Publication Date: 24.02.2005 International Filing Date: 18.08.2004
IPC:
C07D 207/16 (2006.01)
Applicants: TAISHO PHARMACEUTICAL CO., LTD. [JP/JP]; 24-1, Takada 3-chome, Toshima-ku, Tokyo 1708633 (JP) (For All Designated States Except US).
TOMISAWA, Kazuyuki [JP/JP]; (JP) (For US Only).
TATSUTA, Dai [JP/JP]; (JP) (For US Only).
YOSHIDA, Tomomichi [JP/JP]; (JP) (For US Only).
YOKOO, Chihiro [JP/JP]; (JP) (For US Only)
Inventors: TOMISAWA, Kazuyuki; (JP).
TATSUTA, Dai; (JP).
YOSHIDA, Tomomichi; (JP).
YOKOO, Chihiro; (JP)
Agent: SHAMOTO, Ichio; YUASA AND HARA, Section 206, New Ohtemachi Bldg., 2-1, Ohtemachi 2-chome, Chiyoda-ku, Tokyo 1000004 (JP)
Priority Data:
2003-207718 18.08.2003 JP
Title (EN) PROCESS FOR PRODUCTION OF cis-4-FLUORO-L-PROLINE DERIVATIVES
(FR) PROCESSUS DE PRODUCTION DE DERIVES DE CIS-4-FLUORO-L-PROLINE
(JA) cis−4−フルオロ−L−プロリン誘導体の製造法
Abstract: front page image
(EN)A process for producing high-purity cis-4-fluoro -L-proline derivatives highly safely under milder conditions in high yield, characterized by reacting a trans-4-hydroxy -L-proline derivative represented by the general formula [I]: (wherein R1 is an &agr;-amino-protecting group; and R2 a carboxyl-protecting group) with N,N-diethyl-N-(1,1,2,3,3,3-hexafluoropropyl)amine in the presence of a hydrogen fluoride scavenger.
(FR)La présente invention concerne un processus de production de dérivés de cis-4-fluoro-L-proline de haute pureté de manière très sûre dans des conditions légères à haut rendement, qui consiste à faire réagir un dérivés de trans-4-hydroxy-L-proline représenté par la formule générale (I) suivante : (I), (dans cette formule R1 est un groupe de protection amino $g(a) et, R2 est un groupe de protection carboxyle) avec N, N-diéthyl-N-(1, 1, 2, 3, 3, 3, -hexafluoropropyle) amine en présence d'un capteur de fluorure d'hydrogène.
(JA) 本発明は、cis−4−フルオロ−L−プロリン誘導体を、安全性が高く、より緩和な条件で好収率及び高純度品を与える工業的に安価に製造する方法であって、下記式[I] 【化1】 (式中、R1はα−アミノ基の保護基を示し、R2はカルボキシル基の保護基を示す。)で表されるtrans−4−ヒドロキシ−L−プロリン誘導体に、フッ化水素捕捉剤の存在下、N, N - ジエチル - N - (1,1,2,3,3,3−ヘキサフルオロプロピル)アミンを反応させることを特徴とする、cis−4−フルオロ−L−プロリン誘導体の製造方法を提供する。                                                                         
Designated States: AE, AG, AL, AM, AT, AU, AZ, BA, BB, BG, BR, BW, BY, BZ, CA, CH, CN, CO, CR, CU, CZ, DE, DK, DM, DZ, EC, EE, EG, ES, FI, GB, GD, GE, GH, GM, HR, HU, ID, IL, IN, IS, JP, KE, KG, KP, KR, KZ, LC, LK, LR, LS, LT, LU, LV, MA, MD, MG, MK, MN, MW, MX, MZ, NA, NI, NO, NZ, OM, PG, PH, PL, PT, RO, RU, SC, SD, SE, SG, SK, SL, SY, TJ, TM, TN, TR, TT, TZ, UA, UG, US, UZ, VC, VN, YU, ZA, ZM, ZW.
African Regional Intellectual Property Organization (BW, GH, GM, KE, LS, MW, MZ, NA, SD, SL, SZ, TZ, UG, ZM, ZW)
Eurasian Patent Organization (AM, AZ, BY, KG, KZ, MD, RU, TJ, TM)
European Patent Office (AT, BE, BG, CH, CY, CZ, DE, DK, EE, ES, FI, FR, GB, GR, HU, IE, IT, LU, MC, NL, PL, PT, RO, SE, SI, SK, TR)
African Intellectual Property Organization (BF, BJ, CF, CG, CI, CM, GA, GN, GQ, GW, ML, MR, NE, SN, TD, TG).
Publication Language: Japanese (JA)
Filing Language: Japanese (JA)