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Inaperisone hydrochloride, YM-170, HY-770U, HSR-770, HN-770, Inapen, Riran

依那立松 Chemical Name: (?-4'-Ethyl-2-methyl-3-(1-pyrrolidinyl)propiophenone hydrochloride; (?-1-(4-Ethylphenyl)-2-methyl-3-(1-pyrrolidinyl)propan-1-one hydrochloride
CAS No. 90878-85-6, 99323-21-4 (free base)
项目整合开发状态: Phase III
项目研究机构: Abbott (Originator), Yamanouchi (Licensee)
合成路线:By condensation of pyrrolidine (I) with paraformaldehyde (II) and 4-ethylpropiophenone (III) by means of dry HCl in refluxing ethyl acetate.
📌 参考资料/链接:
参考文献标题:Derivs.of 3-pyrrolidinopropiophenone and a proces
文献作者:Itho,Y.; Kato,H.; Koshinaka,E.; Nishino,H.; Ogawa,N.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:EP 0150235

📄 详细内容


合成路线:By condensation of pyrrolidine (I) with paraformaldehyde (II) and 4-ethylpropiophenone (III) by means of dry HCl in refluxing ethyl acetate.

参考文献标题:Derivs.of 3-pyrrolidinopropiophenone and a proces
文献作者:Itho,Y.; Kato,H.; Koshinaka,E.; Nishino,H.; Ogawa,N.(Hokuriku Seiyaku Co.,Ltd.)
参考来源:FR 2559771


合成路线:By condensation of pyrrolidine (I) with paraformaldehyde (II) and 4-ethylpropiophenone (III) by means of dry HCl in refluxing ethyl acetate.

合成路线:The condensation of 2-(dimethylamino)benzyl chloride (I) with 2-mercaptobenzimidazole (II) by means of NaHCO3 in ethanol gives 2-[2-(dimethylamino)benzylthio]benzimidazole (III),which is then oxidized with m-chloroperbenzoic acid (IV) in CHCl3-methanol.

合成路线:The acylation of methylanthranilate (I) with isobutyryl chloride (II) gives 2-isobutyramidobenzoic acid methyl ester (III),which is reduced with LiAlH4 to 2-(isobutylamino)benzyl alcohol (IV).The methylation of (IV) with dimethyl sulfate yields 2-(N-isobutyl-N-methylamino)benzyl alcohol (V),which is treated with SOCl2 to afford the corresponding benzyl chloride (VI).The condensation of (VI) with benzimidazole-2-thiol (VII) by means of NaOH yields 2-[2-(N-isobutyl-N-methylamino)benzylsulfanyl)benzimidazole (VIII),which is finally oxidized with m-chloroperbenzoic acid (MCPBA) as usual.

参考文献标题:Benzimidazole derivs.and antiulcer agents contain
文献作者:Susumu,O.; Masaru,S.; Tomio,Y.; Yutaka,N.; Masatoshi,H.(Nippon Chemiphar Co.,Ltd.)
参考来源:AU 8546409; BE 0903128; CH 665417; DE 3531487; ES 8703142; FR 2569691; GB 2163747; JP 1986060660; JP 1986221175; JP 1986221176; JP 1991223260; JP 1991223261; JP 1991223262; JP 1991227927


合成路线:By condensation of pyrrolidine (I) with paraformaldehyde (II) and 4-ethylpropiophenone (III) by means of dry HCl in refluxing ethyl acetate.
参考文献标题:HSR-770
文献作者:Prous,J.; Castar,J.
参考来源:Drugs Fut 1988,13(4),310


产品链接: CAS No. 90878-85-6››

产品链接: CAS No.99323-21-4››