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首页> 外国专利> METHOD OF OBTAINING 1-PHENOXY-2-OXY-3-OXY-ALKYLAMINOPROPANOV1 The invention relates to a method for the preparation of new, not described in the literature, 1-phenoxy-2-hydroxy-3-oxyalkylaminopropane, which have pharmacological activity and can be used in medicine. Method for producing 1-isopropyl-amino-2-hydroxy-3-

METHOD OF OBTAINING 1-PHENOXY-2-OXY-3-OXY-ALKYLAMINOPROPANOV1 The invention relates to a method for the preparation of new, not described in the literature, 1-phenoxy-2-hydroxy-3-oxyalkylaminopropane, which have pharmacological activity and can be used in medicine. Method for producing 1-isopropyl-amino-2-hydroxy-3-

机译：获得1-苯氧基-2-OXY-3-OXY-烷基酰胺基丙烷的方法本发明涉及一种制备具有药理活性的新的，文献中未记载的1-苯氧基-2-羟基-3-氧烷基氨基丙烷的方法。并可以用于医学。 1-异丙基-氨基-2-羟基-3-的制备方法

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1364280 1-phenoxy, 2-hydroxy, 3-hydroxyalkylamino-propanes BOEHRINGER INGELHEIM GmbH 4 Oct 1971 [5 Oct 1970] 46103/71 Heading C2C [Also in Division A5] Novel compounds of general Formula I and their esters and acid addition salts, where R 1 represents cyano, ethynyl, propargyl, allyl, amino, hydroxymethyl methoxy, hydroxycarbonyl methoxycarbonyl or allyloxy; R 2 represents a hydrogen, chlorine, methyl or cyano; or R 1 and R 2 together represent a 3,4- methylene-dioxy group; R 3 represents hydrogen and R 4 represents a straight or branched hydroxyalkyl group with 3 to 6 C atoms (with the proviso that R 4 is not 1,1-dimethyl-2- hydroxyethyl or 1,2 - dimethyl - 2 - hydroxyethyl when R 1 is 4-amino) are prepared by (1) reacting a compound of Formula II where Z represents the group or -CH.OH-CH 2 -Halogen with an amine NH 2 -R 4 , (2) hydrolysing or hydrogenolysing a compound of Formula IV where G is an acyl or tetrahydropyranyl group, (3) reacting a compound of Formula V with a hydroxyalkyl (with 3 to 6 C atoms)- halide, -tosylate or -mesylate or with a hydroxyaldehyde or hydroxyketone of 3 to 6 C atoms under conditions of reductive alkylation with hydrogen, (4) hydrolysing or hydrogenolysing a compound of Formula VI where Sch is preferably a benzyl carbobenzoxy or acyl group, (5) hydrolysing a compound of Formula VII preferably by using a strong alkali in an aqueous or aqueous/alcoholic medium, (6) hydrolysing or pyrolysing a compound of Formula VIII where R 5 and R 6 are either a hydrogen atom or an alkyl, aralkyl or aryl group, (7) chlorinating a compound Ar-OCH 2 -CHOH-CH 2 -NHR 4 , where Ar represents a phenyl group substituted by RSP1/SP and R 3 preferably by using hydrogen peroxide and a hydrohalic acid, (8) reducing a compound II in which Z is CO-CH 2 -NHR 4 or CHOH-CO-NHR 4 , (9) reacting by known methods a compound X in which A is halogen, aldehyde, amide, oxime, haloalkyl nitro or alkoxy carbonyl to form a compound I in which R 1 is cyano, amino hydroxymethyl, or hydroxycarbonyl, or (10) reacting by known methods a compound X1 in which B is aldehyde or amino to form a compound I in which R 2 is other than hydrogen. Compounds I may be formed as their optical isomers. Acetates and propionates of compounds I may be formed by conventional procedures. Compounds I show #-adrenolytic activity and blood-pressure decreasing properties and form with a carrier or excipient a pharmaceutical composition which may be administered orally rectally or parenterally. The compositions may include coronary dilators, sympathicominetics cardiac glycosides or tranquillizers and in particular 2,6-bis-(diethanolamino-)-4,8-dipiperidino-pyrimido [5,4-d]-pyrimidine.
机译：1364280 1-苯氧基，2-羟基，3-羟基烷基氨基丙烷BOEHRINGER INGELHEIM GmbH 1971年10月4日[1970年10月5日] 46103/71标题C2C [也在A5分部中]通式I的新型化合物及其酯和酸加成盐，其中R 1代表氰基，乙炔基，炔丙基，烯丙基，氨基，羟甲基甲氧基，羟羰基甲氧基羰基或烯丙氧基; R 2代表氢，氯，甲基或氰基; R 1和R 2一起表示3，4-亚甲基二氧基。 R 3代表氢，R 4代表具有3至6个C原子的直链或支链羟烷基（前提是R 4不是1,1-二甲基-2-羟乙基或1,2-二甲基-2-羟乙基（1是4-氨基）是通过（1）使Z代表基团或-CH.OH-CH 2-卤素的式II化合物与胺NH 2 -R 4反应制备的;（2）使化合物水解或氢解式IV的化合物，其中G是酰基或四氢吡喃基，（3）使式V的化合物与羟烷基（具有3至6个C原子）-卤化物，-甲苯磺酸酯或-甲磺酸酯或与3-6的羟醛或羟基酮反应在氢还原烷基化的条件下，C原子;（4）水解或氢解式VI的化合物，其中Sch优选为苄基碳苯甲酰基或酰基，（5）水解式VII的化合物，优选通过在水溶液中使用强碱进行水解或水/醇介质，（6）水解或热解式VIII的化合物R 5和R 6是氢原子或烷基，芳烷基或芳基，（7）氯化化合物Ar-OCH 2 -CHOH-CH 2 -NHR 4，其中Ar表示被R 1 和R 3，最好使用过氧化氢和氢卤酸，（8）还原Z为CO-CH 2 -NHR 4或CHOH-CO-NHR 4的化合物Ⅱ，（9）通过已知方法是，化合物A中的A为卤素，醛，酰胺，肟，卤代烷基硝基或烷氧羰基，以形成化合物I，其中R 1为氰基，氨基羟甲基或羟羰基，或（10）通过已知方法反应其中B为醛或氨基的X1形成其中R 2为氢以外的化合物I。化合物I可以作为它们的旋光异构体形成。化合物I的乙酸酯和丙酸酯可以通过常规方法形成。化合物I表现出＃肾上腺素分解活性和降低血压的性质，并与载体或赋形剂一起形成可经直肠或肠胃外给药的药物组合物。所述组合物可以包括冠状动脉扩张剂，交感神经药强心苷或镇定剂，尤其是2，6-双-（二乙醇氨基-）-4，8-二哌啶子基-嘧啶基[5，4-d]-嘧啶。

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