公开(公告)号：US4734509A

公开(公告)日：1988-03-29

申请号：US854537

申请日：1986-04-22

申请人： Jacob Herzig ,  Ben Z. Weiner ,  Stephan Cherkez ,  Abraham Antebi

发明人： Jacob Herzig ,  Ben Z. Weiner ,  Stephan Cherkez ,  Abraham Antebi

IPC分类号： C07D233/54 ,  C07D233/64

CPC分类号： C07D233/64

摘要： 4(5)-Hydroxymethyl-5(4)-methylimidazole (MHI) is prepared by a process comprising the steps of:(a) reacting 4-methylimidazole (MI) with from 1.05 to 1.1 moles of formaldehyde or an equivalent amount of paraformaldehyde per mole of MI, in a concentrated aqueous NaCl solution in the presence of a catalytically effective amount of a strong inorganic base, at a temperature from about 20.degree. to about 60.degree. C.;(b) neutralizing the reaction mixture with concentrated aqueous hydrochloric acid to a pH of 8.5-8.9 to obtain a precipitate of MHI free base; and(c) separating the precipitate thus obtained from the aqueous solution and washing it with cold water or acetone.The MHI free base thus obtained can further be converted to an acid addition salt thereof.

摘要翻译： 4（5） - 羟甲基-5（4） - 甲基咪唑（MHI）通过包括以下步骤的方法制备：（a）使4-甲基咪唑（MI）与1.05-1.1摩尔甲醛或当量的多聚甲醛 在约20℃至约60℃的温度下，在催化有效量的强无机碱的存在下，在浓的NaCl水溶液中，每摩尔MI。 （b）用浓盐酸水溶液中和反应混合物至pH 8.5-8.9，得到游离碱的游离碱沉淀物; 和（c）从水溶液中分离由此获得的沉淀物并用冷水或丙酮洗涤。 由此获得的MHI游离碱可进一步转化为其酸加成盐。

公开(公告)号：US4889929A

公开(公告)日：1989-12-26

申请号：US30280

申请日：1987-03-26

申请人： Jacob Vaya ,  David Ladkani ,  Clara Schoenberger ,  Joseph Kaspi ,  Gad Salemnick ,  Haim Yellin ,  Stephan Cherkez

发明人： Jacob Vaya ,  David Ladkani ,  Clara Schoenberger ,  Joseph Kaspi ,  Gad Salemnick ,  Haim Yellin ,  Stephan Cherkez

IPC分类号： C07D499/08 ,  C07D499/00 ,  C07D499/04 ,  C07D499/46 ,  C07D499/60 ,  C07D499/64 ,  C07D499/68

CPC分类号： C07D499/00 ,  Y02P20/55

摘要： Process for the preparation of 1'-ethoxy carbonyloxy ethyl esters of penicillins, wherein a compound of the formula ##STR1## in which A is phenyl, phenoxy or 4-hydroxyphenyl, B is hydrogen, an amino group or a protected amino group and Z is hydrogen or a cation selected from the group of alkali metal, tri (lower alkyl ) ammonium and tetra (lower alkyl) ammonium, is reacted with 1-bromoethyl ethyl carbonate in an organic solvent and when B is a protected amino group the protecting group is split off to yield a primary amino group.There are also provided novel compounds of the formula ##STR2## in which Ph is phenyl and R is CH.sub.3 -- or C.sub.2 H.sub.5 --.

摘要翻译： 制备青霉素1'-乙氧基羰基氧基乙酯的方法，其中A为苯基，苯氧基或4-羟基苯基，B为氢，氨基或被保护的氨基的式“IMAGE”的化合物和Z 是氢或选自碱金属，三（低级烷基）铵和四（低级烷基）铵的阳离子在有机溶剂中与1-溴乙基碳酸乙酯反应，当B是被保护的氨基时，保护基 被分离以产生伯氨基。 还提供了新颖的式（IMAGE）化合物，其中Ph是苯基，R是CH 3 - 或C 2 H 5 - 。