RGH-5279
Chemical Name: (-)-(13aR,13bS)-13a-Ethyl-2,3,5,6,13a,13b-hexahydro-1H-indolo[3,2,1-de]pyrido[3,2,1-ij][1,5]naphthyridine-12-carboxylic acid 2-acetoxyethyl ester hydrochloride
项目整合开发状态: Preclinical
项目研究机构: Gedeon Richter (Originator)
合成路线:Transesterification of l,l-trans apovincaminic acid methyl ester (I) with ethylene glycol at 120 C in the presence of potassium tert-butoxide furnished the hydroxyethyl ester (II).Subsequent acetylation of (II) with Ac2O in pyridine gave the corresponding acetoxyethyl ester,which was isolated as the hydrochloride salt upon treatment with HCl in isopropanol.
📌 参考资料/链接:
参考文献标题:Trans apovincaminic acid ester derivs.as drugs
文献作者:Sz醤tay,C.; Moldvai,I.; Vedres,A.; Incze,M.; Kreidl,J.; Czibula,L.; Farkas,J.; Deutschn?Juh醩z,I.; Gere,A.; Pellioniszn?Par骳zai,M.; Lapis,E.; Szekeres,A.; Z醞ern?Bal醶s,M.; Sarkadi,A.; et al.(Gedeon Richter Ltd.)
参考来源:EP 0876367; JP 2000502676; US 6093720; WO 9723481