C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 498/22 (2006.01) A61K 31/505 (2006.01) C07D 475/04 (2006.01) C07D 487/14 (2006.01)
Patent
CA 2056433
The present invention concerns a new process for preparing diastereoisomers derived from tetrahydrofolic acid. By the reaction of (i) (6RS)-folinic acid or one of its salts or (ii) 5,10-methenyl-5,6,7,8-tetrahydrofolic acid with HCOOH at a pH of 2.0-2.6, a precipitate is obtained consisting of a mixture of two diastereoisomers with an orthoamide structure and the formulae (III) and (IV) where R is the p-benzoyl-(L)-glutamic radical, in a molar ratio (IV/III) of about 7/3, with compound (III) of "natural" configuration and compound (IV) of "non-natural" configuration. Pure compound (IV) is isolated from said precipitate and pure compound (III) from the corresponding filtrate. From compound (III) and (IV) are prepared the diastereoisomers of the reduced folates and their natural and non-natural configuraton salts.
-39- A B R E G E La présente invention à trait à un nouveau procé- dé de préparation de diastéréoisomères dérivant de l'acide tétrahydrofolique. Par réaction de (i) l'acide (6RS)-folinique ou de l'un de ses sels, ou (ii) de l'acide 5,10-méthényl-5,6,7,8-tétrahydrofolique, avec HCOOH à pH 2,0-2,6 on obtient un précipité constitué par un mélange de deux diastéréoisomères de structure orthoamide et de formules : Image et Image (III) (IV) où R représente le reste p-benzoyl-(L)-glutamique, dans un rapport molaire IV/III d'environ 7/3, le composé III étant de configuration dite naturelle et le composé IV de configuration dite non-naturelle. On isole le composé IV pur dudit précipité, et le composé III pur du filtrat correspondant. A partir du composé III et respectivement IV on prépare les diastéréoisomères des folates réduits et de leurs sels de configuration naturelle, et respectivement non-naturelle.
Marazza Fabrizio
Melera Attilio
Viterbo Rene
Marazza Fabrizio
Melera Attilio
Sapec S.a.
Sim & Mcburney
Viterbo Rene
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