Facile synthesis of 1,2,4,5-tetrahydro-1,4-benzodiazepin-3-ones <i>via</i> cyclization of <i>N</i>-alkoxy α-halogenoacetamides with <i>N</i>-(2-chloromethyl)aryl amides
作者:Qiaomei Jin、Dongjian Zhang、Jian Zhang
DOI:10.1039/c9ob02260k
日期:——
A facile and efficient cyclization of N-alkoxy α-halogenoacetamides with N-(2-chloromethyl)aryl amides has been achieved for rapid access to 1,2,4,5-tetrahydro-1,4-benzodiazepine-3-one derivatives (up to 95% yield). The intriguing features of this intermolecular cyclization include its mild reaction conditions and easy handling for scalable synthesis.
Cephalosporins having a carbamoylalkoxyiminoarylacetamido group at
申请人:Glaxo Laboratories, Ltd.
公开号:US04385177A1
公开(公告)日:1983-05-24
Antibiotic compounds of the general formula ##STR1## [wherein R is a phenyl, thienyl or furyl group; R.sup.a and R.sup.b, which may be the same or different, are each selected from hydrogen, C.sub.1-4 alkyl, C.sub.2-4 alkenyl C.sub.3-7 cycloalkyl, phenyl, naphthyl, thienyl, furyl, carboxy, C.sub.2-5 alkoxycarbonyl and cyano, or R.sup.a and R.sup.b together with the carbon atom to which they are attached from a C.sub.3-7 cycloalkylidene or cycloalkenylidene group; R.sup.c is hydrogen or lower alkyl; R.sup.d is hydroxy, lower alkoxy, aralkoxy or aryloxy; m and n are each 0 or 1 such that the sum of m and n is 0 or 1; and P is selected from a hydrogen atom, a halogen atom and various organic groups] and non-toxic derivatives thereof.