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项目整合精选>>>Pilocarpine hydrochloride, KSS-694, MGI-647, Pilobuc, Pilocar, Isopto carpine, Spersacarpin, Pilo, Isopto-pilocarpine, Pilocarpina lux, Pilogel, PilaSite(sustained release), Salagen, Pilopine HS
Pilocarpine hydrochloride, KSS-694, MGI-647, Pilobuc, Pilocar, Isopto carpine, Spersacarpin, Pilo, Isopto-pilocarpine, Pilocarpina lux, Pilogel, PilaSite(sustained release), Salagen, Pilopine HS
盐酸毛果芸香碱 毛果芸香碱 硝酸毛果芸香碱Chemical Name: (3S-cis)-3-Ethyldihydro-4-[(1-methyl-1H-imidazol-5-yl)methyl]-2(3H)-furanone monohydrochloride
CAS No. 54-71-7, 92-13-7 (free base), 148-72-1 (mononitrate)
项目整合开发状态: Launched-1947
项目研究机构: MGI (Orphan Drug), Alcon (Originator), Chauvin (Not Determined), Cytokine PharmaSciences (Not Determined), Novartis Ophthalmics (Not Determined), Pfizer (Not Determined), Allergan (Licensee), Chiron (Licensee), Kissei (Licensee), Megapharm (Licensee), MGI
合成路线:The alkylation of pilosine (I) with ethyl chloride (II) by means of LDA in THF gives trans-pilocarpine (III),which is isomerized with LDA in THF,yielding a mixture of cis- and trans-pilocarpine (IV).Finally,this mixture is resolved by crystallization with di-p-toluoyl tartaric acid.
📌 参考资料/链接:
参考文献标题:Pilocarpine analogs as muscarinic agonists
文献作者:Shapiro,G.; Enz,A.
参考来源:Drugs Fut 1992,17(6),489