发明名称 |
PROCESS FOR THE PREPARATION OF A CHIRAL BETA AMINOACID DERIVATIVE AND INTERMEDIATES THEREOF |
摘要 |
<p>It comprises a process for the preparation of sitagliptin, or its pharmaceutically acceptable salts, or its solvates, including hydrates, comprising: a) coupling an halo-2,4,5-trifluorobenzene with a compound of formula (IV) to give N-protected sitagliptin; the coupling being carried out via the formation of an organocupric compound of the halo-2,4,5-trifluorobenzene or, alternatively, via the formation of a organozinc compound of a compound of formula (IV); where R1 is hydrogen or an amino protective group; R2 is an amino protective group; or alternatively R1 and R2 taken together form a phtalimido group; X is Br or I; and Y is Br, I or R3SO3- wherein R3 is (C1-C4)- alkyl, phenyl, or phenyl mono- or disubstituted by a (C1-C4)-alkyl radical; b) submitting the N-protected sitagliptin to a deprotection reaction; and c) optionally its conversion into a pharmaceutically acceptable salt. It also comprises new intermediate compounds useful in such preparation process.</p> |
申请公布号 |
WO2010097420(A1) |
申请公布日期 |
2010.09.02 |
申请号 |
WO2010EP52359 |
申请日期 |
2010.02.24 |
申请人 |
ESTEVE QUIMICA, S.A.;BARTRA SANMARTI, MARTI;RUSTULLET OLIVER, ALBERT;FERNANDEZ HERNANDEZ, SARA;MONSALVATJE LLAGOSTERA, MONTSERRAT |
发明人 |
BARTRA SANMARTI, MARTI;RUSTULLET OLIVER, ALBERT;FERNANDEZ HERNANDEZ, SARA;MONSALVATJE LLAGOSTERA, MONTSERRAT |
分类号 |
C07D487/04 |
主分类号 |
C07D487/04 |
代理机构 |
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代理人 |
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地址 |
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