2-methyl-2-propanethiolate and ketenes, react with imines in the presence of stannous triflate to give the corresponding β-aminocarboxylic thioesters in an anti-selective manner. This method is successfully applied to a diastereoselective synthesis of a carbapenem antibiotic PS-5 intermediate.
锡 (II) 羧酸硫酯烯醇化物由 2-甲基-2-丙硫醇亚锡和烯酮原位形成,在三氟甲磺酸亚锡存在下与亚胺反应,以抗选择性方式生成相应的 β-氨基羧酸硫酯。该方法成功应用于碳青霉烯类抗生素PS-5中间体的非对映选择性合成。
A New Synthetic Route to 1-Aminoalkylphosphonous Acids
作者:Damian Grobelny
DOI:10.1055/s-1987-28133
日期:——
The addition of bis(trimethylsilyl) phosphonite to N-(diphenylmethyl) imines 1 yields bis(trimethylsilyl) 1-(diphenylmethylamino) alkylphosphonites 2, which can be easily converted into 1-(diphenylmethylamino)-alkylphosphonous acids 3 by treatment with aqueous alcohol.
.alpha.-Amino-phosphonous acids for inhibiting bacteria and yeast
申请人:Ciba-Geigy Corporation
公开号:US04147780A1
公开(公告)日:1979-04-03
The present invention relates to new phosphonous acid derivatives, especially to .alpha.-amino-phosphonous acids and processes for their production. The new phosphonous acids are valuable chemotherapeutica in the treatment of pathogenic bacteria, gram-negative bacteria and yeast.
Organophosphorus analogs of biologically active compounds 11. Synthesis of analogs of acyl phosphates based on esters of methylenediphosphorus-containing acids
作者:N. B. Tarusova、Z. S. Novikova、A. A. Prishchenko、G. M. Yakovleva、R. M. Khomutov