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    • 1. 发明公开
    • Synthesis for the preparation of porphobilinogen, the compound as such as stabilized salt and intermediates thereof
    • 一种制备胆色素原的,该化合物本身为稳定的盐和它们的中间体的方法
    • EP1357110A1
    • 2003-10-29
    • EP02009121.1
    • 2002-04-24
    • Neier, Reinhard
    • Neier, ReinhardSoldermann-Pissot, Carole
    • C07D207/32C12P17/10C07F7/18C07C247/12
    • C07D207/337C07F7/1852C07F7/188C12P17/10Y02P20/55
    • The invention relates to a new inventive process sequence of steps a) to e) as claimed in Claim 1 for the preparation of porphobilinogen and intermediates per se as important precursors such as 3-[4-methoxycarbonylmethyl-5-(protected amino-methyl)-1 H-pyrrol-3-yl]-propionic acid methyl ester of formula 7
      wherein R is a protective group,
      and 3-[4-Carboxymethyl-5-(protected amino-methyl)-1 H-pyrrol-3-yl]-propionic acid di-alkali metal salt of formula 8
      and especially 3-[4-carboxymethyl-5-(phenylacetyl-amino-methyl)- 1H-pyrrol-3-yl]-propionic acid di-lithium salt of formula 8a
      and of carboxylate 4-(2-carboxy-ethyl)-3-carboxymethyl-1H-pyrrrol-2-yl-methyl-ammonium of formula 9
      and of phenylacetate 4-(2-carboxy-ethyl)-3carboxymethyl-1 H-pyrrol-2-ylmethyl-ammonium of formula 9a
      and the use thereof for the preparation of porphobilinogen.
    • 本发明涉及到的步骤a)至e)的新发明的工艺顺序,如权利要求1要求保护的用于胆色素原和中间体本身的制备作为重要的前体:例如3- AE4甲氧羰基甲基-5-(保护的氨基 - 甲基) - 式7 worin的R 1个H-吡咯-3-ylÜ - 丙酸甲酯为保护基,和3- AE4羧甲基-5-(保护的氨基 - 甲基)-1H-吡咯-3-ylÜ - 丙酸二碱式的金属盐8 和爱尤其是3- AE4羧甲基-5-(苯基乙酰基氨基 - 甲基) - 式8a的1H-吡咯-3-丙酸ylÜ二锂盐< CHEM>和的羧酸酯4-(2-羧基 - 乙基)式9 和苯乙酸4- -3羧甲基-1H-pyrrrol -2-基甲基 - 铵(2-羧基 - 乙基)-3carboxymethyl -1H-吡咯-2-基甲基 - 铵式9a中及其用于胆色素原的制备中的用途的。