. ;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"/> CHIRAL 4-BORONOPHENYLALANINE (BPA) DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING <Sup>18</Sup>F-LABELED BPA USING SAID DERIVATIVE
首页> 外国专利> CHIRAL 4-BORONOPHENYLALANINE (BPA) DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 18F-LABELED BPA USING SAID DERIVATIVE

CHIRAL 4-BORONOPHENYLALANINE (BPA) DERIVATIVE AND METHOD FOR PRODUCING SAME, AND METHOD FOR PRODUCING 18F-LABELED BPA USING SAID DERIVATIVE

机译:手性4-硼苯丙氨酸(BPA)衍生物及其制备方法,以及利用所述衍生物制备 18 F标记的BPA的方法

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a compound represented by the following formula:; . ;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
机译:化合物本发明涉及下式表示的化合物: 。 ;在公式1中:R是BR 3 R 4 ,BX 3 -或BX 3 < / Sub> - M + (X是卤素; M + 是碱金属离子),R 1 R是甲基,乙基,正丙基,异丙基,正丁基,异丁基,仲丁基,叔丁基,正戊基,苄基,对甲氧基苄基或对硝基苄基,R Sup 2 是氢,苄氧羰基,乙酰基,三氟乙基羧基,叔丁氧羰基,芴基甲氧羰基,三氯乙氧羰基,三氟乙酰基,烯丙氧羰基,苄基,炔丙基氧羰基,苯甲酰基,邻苯二甲酰基,甲苯磺酰基或硝基苯磺酰基,R 3 和< Sup> 4 都与B(硼原子)结合形成一个环作为B的保护基,其中的环选自频哪醇,2,2-二甲基-1,3 -丙二醇,N-甲基二乙醇胺,1,8-二氨基萘,N-甲基亚氨基二乙酸,1,1,1-三羟甲基乙烷和儿茶素,Y为I,F或Br,NO 2 ,N H 2 ,Sn(R 6 3 ,取代或未取代的苯基碘基团或取代或未取代的噻吩基碘基,其中取代基苯基或噻吩基中的一个或多个包括C 1-6 烷基,C 1-6 烷氧基,羟基,氨基和硝基,R 6 是含有1至7个碳原子的烷基。还提供了制备式3的化合物的方法,制备 18 F-标记的BPA和式6的化合物的方法。显示了式3和式6的化合物的结构效果:本发明提供了新颖的BPA衍生物,其可以作为合成 18 F标记的BPA的中间体。; 8 cl,12 ex;формула1-式1

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