. ;In formula 1: R is BR3R4, BX3- or BX3-M+ (X is halogen; M+ is an alkali metal ion), R1 is a methyl, ethyl, n-propyl, iso-propyl, n-butyl, isobutyl, sec-butyl, tert-butyl, n-pentyl, benzyl, a para-methoxybenzyl group or a para-nitrobenzyl group, R2 is hydrogen, benzyloxycarbonyl, acetyl, trifluoroethylcarboxy, tert-butyloxycarbonyl, fluorenylmethyloxycarbonyl, trichloroethoxycarbonyl, trifluoroacetyl, allyloxycarbonyl, benzyl, propargyloxycarbonyl, benzoyl, phthaloyl, toluenesulfonyl or nitrobenzenesulfonyl, R3 and R4 both are combined with B (boron atom) to form a ring serving as a protecting group for B, wherein the ring is selected from the group consisting of a pinacol, 2,2-dimethyl-1,3-propanediol, N-methyldiethanolamine, 1,8-diaminonaphthalene, N-methyliminodiacetic acid, 1,1,1-tris-hydroxymethylethane and catechin, Y is I, F or Br, NO2, NH2, Sn(R6)3, a substituted or unsubstituted phenyl iodine group or a substituted or unsubstituted thienyl iodo group, wherein the substituent(s) of the phenyl group or thienyl includes C1-6 alkyl, C1-6 alkoxy, hydroxy, amino and nitro groups, R6 is an alkyl group containing from 1 to 7 carbon atoms. Also provided is a process for the preparation of a compound of formula 3, a process for preparing 18F-labeled BPA and a compound of formula 6. Structure of the compounds of formula 3 and formula 6 is shown in the claims.;EFFECT: invention provides a novel BPA derivative that can be an intermediate for synthesis 18F-labeled BPA.;8 cl, 12 ex;формула 1 - formula 1"/>
公开/公告号RU2660433C2
专利类型
公开/公告日2018-07-06
原文格式PDF
申请/专利权人 STELLA FARMA KORPOREJSHN;
申请/专利号RU20150118150
发明设计人 TAKENAKA KHIROSI;OKHTA EITIRO;TAGUTI YUSUKE;UEDA SAYURI;ISINO YUKO;NAKASIMA KHIDEKI;UEKHARA KOKHKI;KIRIKHATA MITSUNORI;
申请日2013-10-08
分类号C07F5/04;C07B59;C07C229/36;C07F7/22;
国家 RU
入库时间 2022-08-21 12:35:29