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不对称催化氢化合成D-苯丙氨酸

2017/11/23 10:49:09 次浏览 分类:供方项目

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  项目介绍(简介、技术特点、应用范围、市场前景、效益分析及对投资者要求

  (中文)D-苯丙氨酸是L-苯丙氨酸相对应的非天然氨基酸,在医药领域的用途广泛,在食品、化妆品、生化试剂领域也有广泛应用。D-苯丙氨酸可广泛用于合成治疗老年痴呆症药物、抗肿瘤药物、肽类抗疼止痛药、人体激素类似物、肽类促进剂等,目前主要作为抗糖尿病药那格列那和抗肿瘤药物百士欣的原料。

目前国内的D-苯丙氨酸供应来源主要是化学拆分法生产的产品,质量和产量都不能满足市场需求。鉴于国内外需求日益扩大,新型药物不断出现,D-苯丙氨酸的市场空间极为巨大,具有极强的市场潜力。

本技术以氢气作为氢源、α-乙酰氨基丙烯酸酯及其衍生物为底物,利用催化量的过渡金属和手性膦配体作为催化剂,在高压反应釜中经过一系列置换后,实现底物的不对称氢化。反应具有原子利用率高、反应条件温和、高效、立体选择性好、底物适用范围广等特点。

  (英文)D-Phenylalanine is the non-natural amino acid corresponding to L- Phenylalanine, which is widely used in the areas of food, cosmetics and bio-chemicals. D-Phenylalanine is also used in the synthesis of Alzheimer’s drug, antineoplastic drug, peptides painkiller drug, human hormone analogue and peptides enhancer. Nowadays, it is widely used as the raw material of the antidiabetic drug Nateglinide and the antineoplastic drug Ubenimex.

The domestic supply is racemic resolution of D,L-Phenylalanine, the quality of which can not meet the market requirement. Thus, D-Phenylalanine has a very promising market potential.

In this method, we used hydrogen as hydrogen source, α-acetyl acrylic acid ester and its derivatives as substrates, transitional metals as catalysts and chiral phosphorus as ligand. After a series of reaction processing in high pressure vessels, the asymmetric hydrogenation of the substrates has completed. The reaction has such advantages as high selectivity, high efficiency, atom economy, mild reaction condition, widely ranges of substrates and so on.

 

 
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