申请人:ELI LILLY AND COMPANY
公开号:EP0002937A1
公开(公告)日:1979-07-11
Trans-4a-phenyl and substituted phenyl 2,3,4,4a,5,6, 7,7a-octahydro-1H-2-pyrindines of the formula
wherein:
R1 is hydrogen, C1-C8 alkyl, CH2R3,
in which:
R3 is C2-C7 alkenyl, C3-C6 cycloalkyl, furyl, or tetrahydrofuryl;
R4 and R5 independently are hydrogen, C1-C3 alkyl, or halogen;
n is 0, 1, 2, or 3;
m is 0 or 1, except that when m is o, n is other than O;
X is CO, CHOH, CH=CH, S, or O, except that when n is O, X is other than S or O;
R2 is hydrogen, hydroxy, C1-C3 alkoxy, or C1-C3 alkanoyloxy; and
the non-toxic pharmaceutically acceptable acid addition salts thereof, are useful as analgesic agents having mixed agonist and antagonist properties. The compounds can be prepared by reacting a 4a-aryl-2-substituted-3,4,4a, 5,6,7-hexahydro-2-pyrindine with hydrogen and platinum oxide.
式中的反式-4a-苯基和取代苯基 2,3,4,4a,5,6,7,7a-八氢-1H-2-吡啶
其中
R1 是氢、C1-C8 烷基、CH2R3、
其中
R3 是 C2-C7 烯基、C3-C6 环烷基、呋喃基或四氢呋喃基;
R4 和 R5 分别是氢、C1-C3 烷基或卤素;
n 是 0、1、2 或 3;
m 是 0 或 1,但当 m 是 o 时,n 不是 O;
X是CO、CHOH、CH=CH、S或O,但当n是O时,X不是S或O;
R2 是氢、羟基、C1-C3 烷氧基或 C1-C3 烷酰氧基;以及
其无毒的药学上可接受的酸加成盐,可用作具有混合激动剂和拮抗剂特性的镇痛剂。这些化合物可通过 4a-芳基-2-取代-3,4,4a, 5,6,7-六氢-2-吡啶与氢和氧化铂反应制备。