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classificationCPCAdditional http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/Y02P20-55
classificationCPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentcpc/C07D487-04
classificationIPCInventive http://rdf.ncbi.nlm.nih.gov/pubchem/patentipc/C07D487-04
filingDate 2009-02-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_3f7973402057a8b674260f8cc2ee8649
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_9a2e52c06d41ee0286b47ed7a16cdb66
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_1525caf3710fc4279b5b1b8263a3cfd3
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_5cfe85309490c2e74f1292ece2fe89c4
publicationDate 2010-09-01-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber EP-2223923-A1
titleOfInvention Process for the preparation of a chiral beta aminoacid derivative and intermediates thereof
abstract 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 R 1 is hydrogen or an amino protective group; R 2 is an amino protective group; or alternatively R 1 and R 2 taken together form a phtalimido group; X is Br or I; and Y is r, I or R 3 SO 2 - wherein R 3 is (C 1 -C 4 )-alkyl, phenyl, or phenyl mono- or disubstituted by a (C 1 -C 4 )-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
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