Efficient approaches to S-alkyl-N-alkylisothioureas: syntheses of histamine H3 antagonist clobenpropit and its analogues.
作者信息
Yoneyama Hiroki, Shimoda Ayako, Araki Lisa, Hatano Kouta, Sakamoto Yasuhiko, Kurihara Takushi, Yamatodani Atsushi, Harusawa Shinya
机构信息
Osaka University of Pharmaceutical Sciences, 4-20-1, Nasahara, Takatsuki, Osaka 569-1094, Japan.
出版信息
J Org Chem. 2008 Mar 21;73(6):2096-104. doi: 10.1021/jo702181x. Epub 2008 Feb 16.
PMID:18278935
Abstract
S-Alkyl-N-alkylisothioureas were efficiently synthesized via synthetic approach (A) using 3-phenylpropionyl isothiocyanate (PPI). The utility of the approach was proved by the syntheses of clobenpropit, a potent histamine H(3) antagonist, and its analogues. Alternatively, clobenpropit could be prepared via intramolecular amide cleavage (B) with use of 2-nitrophenylacetyl isothiocyanate (NPAI).
摘要
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