CAS: 2840-29-1; 3-Amino-4-Bromobenzoic Acid

上下游产品

CAS号6319-40-0 4-溴-3-硝基苯甲酸 | CAS号7647-01-0 盐酸 | CAS号46064-79-3 3-氨基-4-溴苯甲酸甲酯 | CAS号6939-93-1 4-溴-1,3-苯二甲酸 | CAS号99-05-8 间氨基苯甲酸 | CAS号204782-96-7 8-溴喹啉-5-甲酸 | CAS号887757-25-7 4-溴-3-氰基苯甲酸 | CAS号56984-35-1 diethyl 4-bromo... | CAS号619-03-4 3,4-二溴苯甲酸

4-溴-3-硝基苯甲酸置于tin(II) Chloride Dihdyrate,溶剂黄146体系中,用 乙酸乙酯 用作溶剂,以86%的收率获得3-氨基-4-溴苯甲酸
参考文献:突变和半合成相结合:一种基于安萨霉素p3的强大合成杂交方法,可用于靶向特异的抗肿瘤药物
标题:突变和半合成相结合:一种基于安萨霉素p3的强大合成杂交方法,可用于靶向特异的抗肿瘤药物
摘要:据报道,四种新的肿瘤特异性叶酸/阿米托星偶联物的获得依赖于基于突变合成和半合成相结合的合成策略.分别通过突变合成或改良的发酵方案制备了两种溴化安那托霉素衍生物,它们是在stille条件下半合成引入烯丙基胺连接基的起点.一系列标准的偶联步骤将蝶酸/谷氨酸/半胱氨酸单元引入到修饰的安托霉素中.所有新的衍生物,包括那些预期在叶酸/阿米托星共轭物内化到癌细胞中以及二硫键还原还原后产生的衍生物,都显示出非常好的至强的抗增殖活性(ic 50 <10 N M)用于不同的癌细胞系.最后,将四种结合物暴露于两种癌细胞系中[子宫颈癌,Kb-3-1(fr +)和肺癌,A-459(fr-)],后者没有膜结合叶酸受体(fr-).所有四种结合物均对fr +癌细胞系表现出强大的抗增殖活性,但对fr-细胞系无活性.所追求的合成策略是基于突变合成和半合成的组合,并被证明对于获取难以通过全合成制备的新的安索霉素衍生物具有强大的作用.
Doi:10.1002/chem.201101640

专利信息

专利号:US-8389767-B2
优先权日:2007-09-04
标题 :Processes and compounds
发明人：STOLLER ANDRE DENIS; JUNG PIERRE JOSEPH MARCEL; GODFREY CHRISTOPHER RICHARD AYLES; MAIENFISCH PETER; ZAMBACH WERNER
权利人:STOLLER ANDRE DENIS; JUNG PIERRE JOSEPH MARCEL; GODFREY CHRISTOPHER RICHARD AYLES; MAIENFISCH PETER; ZAMBACH WERNER; SYNGENTA CROP PROTECTION LLC
摘要:The invention relates to methods of using certain compounds of formula (I), (II) and (III) in the synthesis of an insecticide intermediate of formula (IV), wherein the substituents are as defined in claim 1 , to processes for preparing these compounds, to processes which use these compounds to prepare insecticide intermediates, and to certain novel compounds of formula (II′) and (III′).

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