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标题翻译：氨基醇，其制备方法及其应用，特别是用于有效应用

公开(公告)号：EP0237366B1

公开(公告)日：1989-04-26

申请号：EP87400116.7

申请日：1987-01-19

申请人： JOUVEINAL S.A.

发明人： Aubard, Gilbert , Bure, Jacques , Calvet, Alain Pierre , Gouret, Claude , Grouhel, Agnès Geneviève , Junien, Jean-Louis

IPC分类号： C07C91/16 , C07C103/30 , C07C103/44 , C07C103/737 , C07D295/08 , A61K31/135 , A61K31/10 , A61K31/445

CPC分类号： C07D295/092

摘要： 1. Claims (for the Contracting States : BE, CH, DE, FR, GB, IT, LI, LU, NL, SE) Aminoalcohols of formula see diagramm : EP0237366,P25,F1 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle or, when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links which can have, as the second heteroatom not directly connected to the nitrogen atom, an oxygen, a sulphur or a nitrogen, the latter nitrogen heteroatom possibly carrying an alkyl substituent in C1 to C4 , and their acid addition salts. 1. Claims (for the Contracting States : AT, ES) Process for the preparation of aminoalcohols of formula see diagramm : EP0237366,P26,F2 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle, or when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links and which can comprise, as the second heteroatom not directly linked with the nitrogen atom, an oxygen, a sulphur or a nitrogen, whereby said latter nitrogen heteroatom can carry an alkyl substituent in C1 to C4 and their acid addition salts, characterized in that it comprises : reducing an acid of formula see diagramm : EP0237366,P27,F1 by a boron or aluminium hydride to obtain compounds (la), in which R2 and R3 are hydrogen and for obtaining compounds (lb), in which NR2 R3 form a heterocycle performing a cyclization by reacting a compound (la) with a reagent of formula X-(CH2 )m -R5 -(CH2 )n -X' in which X and X', which can be the same or different, are halogen, R5 is a single valence bond and m and n are integers between 1 and 3, with m + n equal to or greater than 4 and equal to or less than 6, or R5 is an oxygen, a sulphur or NR6 , R6 being H or alkyl in C1 to C4 and m and n are integers between 1 and 3 with m + n equal to or higher than 3 and equal to or lower than 5 and for preparing compounds (lc), in which R3 is alkanoyl, phenylalkanoyl or cycloalkylcarbonyl, acylating a compound (la) with an acylating agent of formula R4 -COX, in which X is a halogen and R4 is the homolog immediately below R3 and for preparing compounds (ld), in which R2 is H and R3 is alkyl, alkenyl, phenylalkyl or cycloalkylalkyl, alkylating a compound (la) using an alkylating agent R3 -X, X being a halogen, or reducing a compound (lc) by a boron or aluminium hydride, or reducing a compound of formula see diagramm : EP0237366,P27,F2 by a boron or aluminium hydride and for preparing compounds (le), in which R2 is alkyl and R3 identical to R2 , reacting a compound (la) with an aldehyde of formula R4 CHO in the presence of formic acid and for preparing compounds (le) in which R2 is alkyl and R3 is alkyl, alkenyl, phenylalkyl or cycloalkylalkyl, reacting a compound (ld) with an aldehyde of formula R4 CHO in the presence of formic acid and, for preparing the acid addition salts, reacting the compounds (l) with an acid. 1. Claims (for the Contracting State GR) Aminoalcohols of formula see diagramm : EP0237366,P28,F1 in which R1 is lower alkyl and R2 is H or lower alkyl, R3 is H, lower alkyl, lower alkenyl, lower phenylalkyl or lower cycloalkylalkyl with 3 to 6 carbon atoms in the cycle or, when R2 is H, lower alkanoyl, lower phenylalkanoyl or cycloalkylcarbonyl having 3 to 6 carbon atoms in the cycle, or R2 and R3 form together with the nitrogen atom to which they are linked, a heterocycle saturated with 5 to 7 chain links which can have, as the second heteroatom not directly connected to the nitrogen atom, an oxygen, a sulphur or a nitrogen, the latter nitrogen heteroatom possibly carrying an alkyl substituent in C1 to C4 , and their acid addition salts.

摘要翻译： 1.索赔（对于缔约国：BE，CH，DE，FR，GB，IT，LI，LU，NL，SE）式的氨基醇见图：EP0237366，P25，F1，其中R1是低级烷基，R2是H 或低级烷基，R 3为H，低级烷基，低级烯基，低级苯基烷基或具有3至6个碳原子的低级环烷基烷基，或当R 2为H时，低级烷酰基，低级烷酰基或低级烷基或R 2和R 3与它们所连接的氮原子一起形成饱和有5至7个链接的杂环，其可以具有不直接与氮原子直接连接的第二杂原子的氧，硫或氮，后者可能在C1至C4中带有烷基取代基的氮杂原子及其酸加成盐。 1.权利要求（对于缔约国：AT，ES）制备式I的氨基醇的方法见图：EP0237366，P26，F2，其中R1是低级烷基，R2是H或低级烷基，R3是H，低级烷基，或者R2为H时，低级链烯基，低级苯基烷基或具有3至6个碳原子的低级环烷基烷基，或R2或R3与氮一起形成时，低级链烷酰基，低级烷酰基或碳原子数3〜6的环烷基羰基它们连接的原子，具有5至7个链键饱和的杂环，并且可以包含与氮原子不直接连接的第二杂原子，氧，硫或氮，其中所述后氮杂原子可以携带 C1至C4中的烷基取代基及其酸加成盐，其特征在于其包括：通过硼氢化铝或氢化铝将还原酸的式为EP0237366，P27，F1，得到化合物（Ia），其中R2和R3为氢和用于获得c 其中NR2 R3通过使化合物（Ia）与式X-（CH 2）m -R 5 - （CH 2）n -X'的试剂反应而形成杂环，其中X和X'，其可以相同或不同，是卤素，R5是单价键，m和n是1和3之间的整数，m + n等于或大于4且等于或小于6，或R5是氧，硫或NR 6，R 6为H或C 1至C 4中的烷基，m和n为1至3的整数，m + n等于或高于3且等于或低于5，并且用于制备化合物（1c）其中R 3是烷酰基，苯基烷酰基或环烷基羰基，用式R 4 -COX的酰化剂酰化化合物（Ia），其中X是卤素，R4是R3下面的同源物，并且用于制备化合物（1d）其中R2是H，R3是烷基，烯基，苯基烷基或环烷基烷基，使用烷基化剂R3-X，X是卤素烷基化化合物（Ia），或用硼还原化合物（1c）或氢化铝，或通过硼氢化铝或氢化铝还原下式的化合物：EP0237366，P27，F2和用于制备化合物（le），其中R 2是烷基，R 3与R 2相同，使化合物（Ia）与在甲酸存在下，式R 4 CHO的醛，并且用于制备其中R 2是烷基和R 3是烷基，烯基，苯基烷基或环烷基烷基的化合物（ⅱ），使化合物（1d）与式R 4 CHO的醛在存在甲酸，并且为了制备酸加成盐，使化合物（1）与酸反应。 1.权利要求（对于缔约国GR）式的氨基醇见图示：EP0237366，P28，F1，其中R1是低级烷基，R2是H或低级烷基，R3是H，低级烷基，低级烯基，低级苯基烷基或低级环烷基烷基在该循环中具有3至6个碳原子，或当R 2为H时，该循环中具有3至6个碳原子的低级烷酰基，低级苯酰基或环烷基羰基，或者R 2和R 3与它们所连接的氮原子一起形成，具有5至7个链接的杂环，其可以具有作为不直接与氮原子直接相连的第二杂原子的氧，硫或氮，后者可在C1至C4中带有烷基取代基的氮杂原子及其酸加成盐。

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