【药物名称】Olanexidine hydrochloride, OPB-2045
化学结构式(Chemical Structure):
参考文献No.34438
标题:Biguanide derivs., manufacturing method thereof, and disinfectants containing the derivs.
作者:Ishikawa, H.; Yasumura, K.; Tsubouchi, H.; Higuchi, Y.; Tamaoka, H. (Otsuka Pharmaceutical Co., Ltd.)
来源:EP 0507317
合成路线图解说明:

OPB-2045 can be obtained by several related ways: 1) The addition of 3,4-dichlorobenzylamine hydrochloride (I) to sodium dicyanamide (II) in refluxing acetonitrile gives 1-(3,4-dichlorobenzyl)-3-cyanoguanidine (III), which is then condensed with octylamine hydrochloride (IV) in refluxing mesitylene. 2) The treatment of S,S'-dimethyl(cyanoimino)dithiocarbonate (V) with aqueous ammonia and further reaction with 3,4-dichlorobenzylamine hydrochloride (I) yields intermediate (III), which is then condensed with (IV) as before. 3) By condensation of 3,4-dichlorobenzylamine hydrochloride (I) with 1-cyano-3-octylguanidine (VI) in refluxing mesitylene.

参考文献No.425226
标题:Synthesis and structure-activity relationships of new disinfectants
作者:Yasumura, K.; Kikuchi, M.; Ishikawa, H.; Ohguro, K.; Tsubouchi, H.
来源:Symp Med Chem 1996,Abst 2-P-3
合成路线图解说明:

OPB-2045 can be obtained by several related ways: 1) The addition of 3,4-dichlorobenzylamine hydrochloride (I) to sodium dicyanamide (II) in refluxing acetonitrile gives 1-(3,4-dichlorobenzyl)-3-cyanoguanidine (III), which is then condensed with octylamine hydrochloride (IV) in refluxing mesitylene. 2) The treatment of S,S'-dimethyl(cyanoimino)dithiocarbonate (V) with aqueous ammonia and further reaction with 3,4-dichlorobenzylamine hydrochloride (I) yields intermediate (III), which is then condensed with (IV) as before. 3) By condensation of 3,4-dichlorobenzylamine hydrochloride (I) with 1-cyano-3-octylguanidine (VI) in refluxing mesitylene.

参考文献No.425227
标题:Synthesis and structure-activity relationships of novel antiseptics
作者:Kikuchi, M.; Ishikawa, H.; Yasumura, K.; Ohguro, K.; Tsubouchi, H.
来源:Bioorg Med Chem Lett 1997,7(13),1721
合成路线图解说明:

OPB-2045 can be obtained by several related ways: 1) The addition of 3,4-dichlorobenzylamine hydrochloride (I) to sodium dicyanamide (II) in refluxing acetonitrile gives 1-(3,4-dichlorobenzyl)-3-cyanoguanidine (III), which is then condensed with octylamine hydrochloride (IV) in refluxing mesitylene. 2) The treatment of S,S'-dimethyl(cyanoimino)dithiocarbonate (V) with aqueous ammonia and further reaction with 3,4-dichlorobenzylamine hydrochloride (I) yields intermediate (III), which is then condensed with (IV) as before. 3) By condensation of 3,4-dichlorobenzylamine hydrochloride (I) with 1-cyano-3-octylguanidine (VI) in refluxing mesitylene.

参考文献No.482254
标题:OPB-2045
作者:Sorbera, L.A.; Casta馿r, J.
来源:Drugs Fut 1999,24(2),151
合成路线图解说明:

OPB-2045 can be obtained by several related ways: 1) The addition of 3,4-dichlorobenzylamine hydrochloride (I) to sodium dicyanamide (II) in refluxing acetonitrile gives 1-(3,4-dichlorobenzyl)-3-cyanoguanidine (III), which is then condensed with octylamine hydrochloride (IV) in refluxing mesitylene. 2) The treatment of S,S'-dimethyl(cyanoimino)dithiocarbonate (V) with aqueous ammonia and further reaction with 3,4-dichlorobenzylamine hydrochloride (I) yields intermediate (III), which is then condensed with (IV) as before. 3) By condensation of 3,4-dichlorobenzylamine hydrochloride (I) with 1-cyano-3-octylguanidine (VI) in refluxing mesitylene.

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