Abstract: Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this processL-amino acids of the formula I and salts thereof, ##STR1## in which R.sup.1 to R.sup.5 are defined as in claim 1 and n is 0 or 1, are obtained according to the invention bya) reacting an optically active S-homoserine lactone of the formula II, ##STR2## with hydrogen chloride in the presence of an alcohol of the formula R.sup.5 --OH to give novel compounds of the formula III, ##STR3## in which R.sup.3, R.sup.4 and R.sup.5 are defined as in formula I, except that R.sup.5 =H, andb) reacting the resulting compound of formula III with a compound of formula IV,R.sup.1 (O).sub.n -R(OR.sup.2).sub.2 (IV)and if desired, hydrolyzing the product to give a compound of formula I, in which R.sup.5 =H.
Abstract: Diphosphonic acids of formula (I), wherein R.sub.1 and R.sub.2 are hydrogen or C.sub.1 -C.sub.4 alkyl; (A) is hydrogen, halogen, hydroxy or C.sub.1 -C.sub.12 alkyl; (B) is a bond, a C.sub.1 -C.sub.8 alkylene chain, a cycloalkylalkylene chain, an alkylene chain substituted by cyclohexyl or cyclopentyl groups, or an aralkyl chain, an alkyl chain containing an heteroatom (O, S or N--CH.sub.3) or an ureido residue --(CH.sub.2).sub.nl --NHCONH--(CH.sub.2).sub.n --with n ranging from 1 to 5, R.sub.3 is hydrogen, C.sub.1 -C.sub.9 alkyl, C.sub.3 -C.sub.6 cycloalkyl, benzyl, phenyl or p-methoxybenzyl; (C) is C.sub.1 -C.sub.5 alkyl, phenyl or an aralkyl chain; R.sub.4 is hudrogen, C.sub.1 -C.sub.5 alkyl or an amino group optionally substituted by alkyl, phenyl, benzyl, p-methoxybenzyl, acyl, amminoacidic or peptide groups; R.sub.5 and R.sub.6 are 2-haloethyl or together form a 1-aziridinyl residue, are useful as antitumor agent.
Abstract: Disclosed is a phosphoric acid ester derivative represented by the general formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are each lower alkyl, X.sup.1 and X.sup.2 are the same or different and are each a hydrogen atom or halogen atom, and Y is an oxygen atom or sulfur atom. The phosphoric acid ester derivatives of the present invention are usable as insecticides and miticides having excellent residual activity and low toxicity to warm blooded animals.
Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents, are provided which have the structure ##STR1## wherein R.sup.2 is a metal ion, lower alkyl or H; R.sup.3 is a metal ion or lower alkyl;R is R.sup.1 --(CH.sub.2).sub.n --, R.sup.1 --(CH.sub.2).sub.m --O-- or R.sup.1 --(CH.sub.2).sub.m --OCH.sub.2 --, wherein n is 1 to 4 and m is 0 to 3, andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein.New intermediates, new methods of preparation and a method for using such compounds to inhibit cholesterol biosynthesis are also provided.