首页> 外国专利> Process for preparing compounds of metanodibenzosuberano 10,11 - and pharmaceutically acceptable salts of the compounds, method for Preparing information intermediaries in this procedure; triclorhidratos crystalline (2R) - anti - 5 - {3 - 4 - (1 - difluorometanodibenzo - 5 - 1 - il) piperacin

Process for preparing compounds of metanodibenzosuberano 10,11 - and pharmaceutically acceptable salts of the compounds, method for Preparing information intermediaries in this procedure; triclorhidratos crystalline (2R) - anti - 5 - {3 - 4 - (1 - difluorometanodibenzo - 5 - 1 - il) piperacin

机译:制备间二苯并亚苏打灵10,11的化合物及其化合物的可药用盐的方法,该方法中信息中间体的制备方法;三角藻(2R)-抗-5-{3-[4-(1-二氟甲基二苯并菲-5-1-il)哌嗪

摘要

The preparation procedure of 10.11-dibenzofuran derivatives (alternative substitutes) is described and the requirements are put forward. The present document also provides an intermediate document for this procedure. The procedure includes the preparation of formula compound (1), where a is - ch2-ch2 -.-CH2-CHRA-CH2-CH2-CHRA-CH2-CH2R1 is oh; R1 is h, F, CL or br; R2 is h, F, CL or br; R3 is isobutylene or phenyl, respectively, substituted by F, Cl, Br, CF3, CN, NO2 or ochf2; or pharmaceutically acceptable salts, whose characteristics include (a) reacting a formula compound (2) with a nuclear power source to form a nuclide source. 1. Formula compound (3);(b) Reacting a formula compound (3) with pyridine to provide a formula compound (4);(c) Reducing formula compound (4) to provide a formula compound (5);(d) A formula compound (5) reacts with: (1) formula (6) of an epoxy compound, wherein R3 is the defined integer and N is the integer 1 or 2; or (2) formula (7) of a halogenated compound: X1 - (CH2) m-o-r3, wherein R3 is previously defined, X1 is halogenated compound and M is 2, 3 or 4; And (E) optionally producing a pharmaceutically acceptable salt from a formula compound (6) or (7).
机译:描述了10.11-二苯并呋喃衍生物(替代品)的制备过程,并提出了要求。本文档还提供了此过程的中间文档。该方法包括制备式化合物(1),其中a为-ch2-ch2 --.- CH2-CHRA-CH2-CH2-CHRA-CH2-CH2R1为OH; R1是h,F,CL或br; R 2为h,F,CL或br; R3分别是被F,Cl,Br,CF3,CN,NO2或ochf2取代的异丁烯或苯基;或其药学上可接受的盐,其特征包括(a)使式化合物(2)与核动力源反应形成核素源。 1.式化合物(3);(b)使式化合物(3)与吡啶反应以提供式化合物(4);(c)还原式化合物(4)以提供式化合物(5);(d)式化合物(5)与以下化合物反应:(1)环氧化合物的式(6),其中R 3为定义的整数,N为整数1或2;或(2)卤代化合物的式(7):X 1-(CH 2)m -o-r 3,其中R 3是预先定义的,X 1是卤代化合物,M是2、3或4;或并且(E)任选地由式化合物(6)或(7)产生药学上可接受的盐。

著录项

  • 公开/公告号AR037068A1

    专利类型

  • 公开/公告日2004-10-20

    原文格式PDF

  • 申请/专利权人 ELI LILLY AND COMPANY;

    申请/专利号AR2000P102679

  • 发明设计人

    申请日2000-05-31

  • 分类号C07D295/06;C07D295/00;C07D215/20;

  • 国家 AR

  • 入库时间 2022-08-21 23:12:21

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