CAS: 135042-12-5; (2R,4R)-1-(Tert-Butoxycarbonyl)-4-Hydroxypyrrolidine-2-Carboxylic Acid

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N-α-Tert-Butyloxycarbonyl-Cis-4-Hydroxy-D-Proline Ethyl Ester置于lithium Hydroxide体系中,用 乙醇 用作溶剂,化学反应 2.0H,反应生成N-Boc-顺式-4-羟基-D-脯氨酸
参考文献:一种通过 Wittig 型反应制备 α,β-二脱氢氨基酸衍生物的新合成方法.(2S,4S)-和 (2R,4R)-4-羟基脯氨酸的合成
标题:一种通过 Wittig 型反应制备 α,β-二脱氢氨基酸衍生物的新合成方法.(2S,4S)-和 (2R,4R)-4-羟基脯氨酸的合成
摘要:在三丁基膦和碱的存在下,N-Boc-和nz-α-甲苯磺酰基甘氨酸乙酯与各种醛反应,以非常好的收率提供相应的α,β-二脱氢氨基酸衍生物,具有高(z)选择性.此外,通过本方法制备的(4S)-和(4R)-2-(N-Boc-氨基)-4,5-异亚丙基二氧基-2-戊烯酸乙酯转化为(2S,4S)-和(2R,4R) )-4-羟脯氨酸,分别.
Doi:10.1246/bcsj.75.2517

专利信息

专利号:WO-2006038119-A1
优先权日:2004-10-08
标题:Stereoselective synthesis of n-protected alkoxy prolines
发明人：VRIEZE DEREK CLINTON
权利人:WARNER LAMBERT CO; VRIEZE DEREK CLINTON
摘要:A process for preparing optically-active N-protected alkoxy prolines, including (2R,4R)-4-methoxy-pyrrolidine-1,2-dicarboxylic acid 1-tert-butyl ester is disclosed. The N-protected alkoxy prolines are useful for preparing various serine protease factor Xa inhibitors, which are useful for treating diseases associated with abnormal thrombosis.