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    • 45. 发明授权
    • Production of intermediates for enzyme inhibitors
    • 生产酶抑制剂的中间体
    • US4325877A
    • 1982-04-20
    • US160057
    • 1980-06-16
    • Brian W. MetcalfJerry L. Adams
    • Brian W. MetcalfJerry L. Adams
    • C07C69/66C07C69/716C07C69/74C07C117/08
    • C07C247/00C07C323/00
    • 5-Amino-4-oxo-pentanoic acids of the formula ##STR1## wherein R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is H or akyl of 1-4 carbon atoms; and R.sub.2 is H or alkyl or 1-4 carbon atoms or benzyl, which are intermediates to ACE inhibitors or elastase inhibitors, are produced by reacting a 1-(methylthio)-1-methylsulfinyl)-2-R.sub.1 -ethylmetal with an ester of a 3-R-acrylic acid; optionally R.sub.2 -alkylating the thus-produced ester enolate anion of 4-(methylsulfinyl)-4-(methylthio)-5-R.sub.1 R-pentanoic acid followed by splitting off of methylsulfinic acid; reacting the thus-produced 2-R.sub.2 -5-R.sub.1 -4-(methylthio)-3-R-4-pentenoic acid ester with a source of Br.sup.+ to produce a 5-bromo-substituted acid or ester thereof otherwise corresponding to the desired 5-amino-4-oxo-pentanoic acid; and replacing the bromine atom with an amino group, e.g., via the corresponding 5-azido- and 5-N-acylamino- compounds, with hydrolysis of the ester group, if still remaining.
    • 其中R是CF 3,CHF 2或CH 2 F的5-氨基-4-氧代 - 戊酸; R1是H或1-4个碳原子的烷基; R2是H或烷基或1-4个碳原子,或作为ACE抑制剂或弹性蛋白酶抑制剂的中间体的苄基是通过使1-(甲硫基)-1-甲基亚磺酰基)-2-R 1 - 乙基金属与 3-R-丙烯酸; 任选地将4-(甲基亚磺酰基)-4-(甲硫基)-5-R1R-戊酸由此产生的酯烯醇化物阴离子R2-烷基化,随后分解出甲基亚磺酸; 使由此产生的2-R2-5-R1-4-(甲硫基)-3-R-4-戊烯酸酯与Br +源反应,产生5-溴取代的酸或酯,否则对应于所需的 5-氨基-4-氧代 - 戊酸; 并且如果仍然存在,则通过相应的5-叠氮基 - 和5-N-酰基氨基化合物用氨基取代溴原子,同时酯基的水解。
    • 46. 发明授权
    • .alpha.Acetylene and .alpha.-vinyl derivatives of amino acids
    • α乙炔和氨基酸的α-乙烯基衍生物
    • US4323704A
    • 1982-04-06
    • US225503
    • 1981-01-16
    • Brian W. MetcalfMichel JungCharles Danzin
    • Brian W. MetcalfMichel JungCharles Danzin
    • C07C103/52C07C101/28C07C103/68C07C125/065C07C125/073C07C129/12
    • Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.b can be the same or different; with the provisos that when R.sub.2 is hydrogen, R.sub.1 is --C.tbd.CH; when A is ethylidene, R.sub.2 is hydrogen; and when R.sub.a is ##STR6## A is methylene; and pharmaceutically acceptable salts and individual optical isomers thereof.
    • 新颖的式(Ⅰ)化合物,其中A是亚甲基,亚乙基或亚乙基; R1是-C3BCH或-CH = CH2; R2是氢或COR,其中R是羟基,1至8个碳原子的直链或支链烷氧基,-NR4R5,其中R4和R5分别是氢或1-4个碳原子的直链或支链低级烷基或 其中R 6是氢,1至4个碳原子的直链或支链低级烷基,苄基或对羟基苄基; R a是氢,其中烷基部分具有1至4个碳原子并且是直链或支链的烷氧基羰基,其中烷氧基部分具有1至4个碳原子并且是直链或支链或其中R7被选定 由氢,1至4个碳原子的直链或支链低级烷基,苄基和对羟基苄基; 并且Rb具有与Ra所定义的相同的含义,不同之处在于Rb不是< IMAGE>并且Ra和Rb可以相同或不同; 条件是当R2是氢时,R1是-C3BCH; 当A为亚乙基时,R 2为氢; 而当Ra为亚甲基时, 及其药学上可接受的盐和单独的光学异构体。