Synthetic applications of bis(iminophosphoranes). One-pot preparation of rigid bicyclic guanidines
摘要:
A one-pot synthesis of [6 + 6], [6 + 7], and [6 + 8] bicyclic guanidines based on a new method of dihydropyrimido annelation, which involves reaction of bis(iminophosphoranes) with aryl isocyanates or isothiocyanates is described. The method is also applicable for the preparation of chiral bicyclic guanidines.
Synthetic applications of bis(iminophosphoranes). One-pot preparation of rigid bicyclic guanidines
摘要:
A one-pot synthesis of [6 + 6], [6 + 7], and [6 + 8] bicyclic guanidines based on a new method of dihydropyrimido annelation, which involves reaction of bis(iminophosphoranes) with aryl isocyanates or isothiocyanates is described. The method is also applicable for the preparation of chiral bicyclic guanidines.
An aminocarboxylic acid derivative represented by the formula
wherein R, and R2, independently from each other, represent a hydrogen atom or an alkyl group which may have a substituent, and Y represents -NH- or -S-, provided that when Y represents -NH-, at least one of R, and R2 represents an alkyl group which may have a substituent. This compound has excellent inhibitory activity on dipeptidase in animals, and is useful for administration in combination with carbapenem antibiotics.
一种由式表示的氨基甲酸酯衍生物
其中 R 和 R2 各自代表氢原子或可带有取代基的烷基,Y 代表-NH-或-S-,但当 Y 代表-NH-时,R 和 R2 中至少有一个代表可带有取代基的烷基。该化合物对动物体内的二肽酶具有极佳的抑制活性,可与碳青霉烯类抗生素联合使用。
Synthetic applications of bis(iminophosphoranes). One-pot preparation of rigid bicyclic guanidines
作者:Pedro Molina、Mateo Alajarin、Angel Vidal
DOI:10.1021/jo00059a015
日期:1993.3
A one-pot synthesis of [6 + 6], [6 + 7], and [6 + 8] bicyclic guanidines based on a new method of dihydropyrimido annelation, which involves reaction of bis(iminophosphoranes) with aryl isocyanates or isothiocyanates is described. The method is also applicable for the preparation of chiral bicyclic guanidines.