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1. 发明授权

US3417098A Phosphoryl derivatives of 4-imidazolidones 失效
标题翻译： 4-咪唑啉酮的磷酰衍生物
公开(公告)号：US3417098A
公开(公告)日：1968-12-17
申请号：US43906865
申请日：1965-03-11
申请人： KUHLMANN ETS
发明人： JESUS ANATOL
IPC分类号： C07D233/88 , C07F9/22 , C07F9/24 , C07F9/6506
CPC分类号： C07F9/65067 , C07F9/222 , C07F9/2458
摘要： The invention comprises compounds of the general formulae and of the general formulae where X is hydrogen or an alkali metal, and R is hydrogen or an XOOC-alkyl group. The compounds I may be prepared by condensing a compound of the general formula (Aryl.CH2O)2-P(=O).N(Me)CN, where Aryl is an aryl or substituted aryl group and Me is an alkali metal, with a mineral acid salt of an amino-acid ester of the general formula H2N.CH(R).COOR1, where R1 is an alkyl group. The condensation may be effected in the presence of an organic solvent. Compounds of Formulae III and IV may be obtained by subjecting the esters I to hydrolysis followed by hydrogenolysis, for example in the presence of palladium black, of the diester products thus obtained. Examples are given in which R is hydrogen and carboxyalkyl respectively and the phosphoryl cyanamide starting materials are obtained as in Specification 937,931 from dibenzyloxyphosphoryl - S - methyl - isothiourea. Acyclic products are obtained by alkaline hydrolysis of the compounds I. These are then cyclized by ethanolic HCl before hydrogenolysis which in the absence of excess alkali yields the cyclic products IV and in alkaline solution yields the acyclic products III which can also be obtained from the products IV by treatment with dilute alkali as in Specification 937,931. The examples also disclose the preparation of calcium salts of phosphoryl - a - guanidino - glutaric acid, and phosphoryl - a - guanidino - succinic acid. The compounds of the Formulae III and IV and their salts have antifatigue properties.

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