氯化3-溴-6-甲基哒嗪正离子 | 50359-19-8

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 氯化3-溴-6-甲基哒嗪正离子
• 英文名称: D(-)-α-amino-p-hydroxy-α-phenylacetic acid chloride hydrochloride
• 英文别名: D(-)-α-amino-α-(p-hydroxyphenyl)acetyl chloride hydrochloride；D-(-)-2-(p-hydroxyphenyl)glycyl chloride hydrochloride；D(-)-α-(p-hydroxyphenyl) glycinechloride hydrochloride；D(-)-α-amino-4-hydroxy-α-phenylacetic acid chloride hydrochloride；(2-Chloro-1-(4-hydroxyphenyl)-2-oxoethyl)ammonium chloride；2-amino-2-(4-hydroxyphenyl)acetyl chloride;hydrochloride
• CAS: 50359-19-8
• 化学式: C₈H₈ClNO₂*ClH
• 分子量: 222.071
• InChiKey: MRFJAULKKHVIGF-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.58
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.12
• 拓扑面积：
  64.9
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  氯化3-溴-6-甲基哒嗪正离子 生成 amoxycillin trihydrate
  参考文献：
  名称：

  Method for synthesis of penicillin

  摘要：

  本发明涉及一种合成青霉素的方法，通过在不溶性弱碱性树脂的存在下，反应6-氨基青霉酸硅酯和羧酸卤化物来合成青霉素。

  公开号：

  US04251442A1
• 作为产物：
  描述：

  2-(4-Hydroxyphenyl)-2-(propan-2-yloxycarbonylamino)acetic acid 、 氯化亚砜 、 三氯乙酸 生成 氯化3-溴-6-甲基哒嗪正离子
  参考文献：
  名称：

  ASCHER, G.;RIEDL, K.

  摘要：

  DOI：

文献信息

• Process for the preparation of cefadroxil
  申请人：Orchid Chemicals & Pharmaceuticals Limited

  公开号：US20040077849A1

  公开（公告）日：2004-04-22

  The present invention relates to an improved process for the preparation of cefadroxil of the formula (I), more particularly, the present invention relates to an improved process for the preparation of cefadroxil having water content in the range of 4-5%. 1

  本发明涉及一种改进的制备cefadroxil (I)的方法，更具体地，本发明涉及一种改进的制备水含量在4-5%范围内的cefadroxil的方法。
• Process for the preparation of 6- D-alpha-amino-(p-hydroxyphenyl)-acetamido penicillanic acid
  申请人：GIST-BROCADES N.V.

  公开号：EP0001133A1

  公开（公告）日：1979-03-21

  Process for the preparation of / D-a-amino-p- hydrox- yphenylacetamido/ groups containing penicillanic acid and cephalosporanic acid derivatives, comprising the acylation of a compounds of the formulae: and/or or and/or wherein R1, R2, and R3 represent the same or a different group and may be selected from a lower alkyl, benzyl, cycloalkyl or phenyl-group and preferably lower alkyl and more preferably a methyl group and wherein X represents a residue selected from the group consisting of hydrogen, acetoxy or a fivemembered heterocyclic thio residue, containing heteroatoms selected from nitrogen, oxygen and/or sulphur and optionally substituted by lower alkyl and wherein an eventually present -NH- radical has optionally been silylated, which compound is previously prepared by the reaction of -6-aminopenicillanic acid or 7-aminocephalosporanic acid or its 3-methyl modifications with at least one equivalent and preferably about 2 with respect to 6-APA, 7-ACA or 7-ADCA and about 3 equivalents with respect to other 3-methyl modifications of 7-ACA of a tri(lower)alkyl silyl groups supplying agent in a dry inert, water insoluble solvent, such as methylene chloride, by rapid mixing of a pre-cooled solution of the compound of formula I-IV with a pre-cooled reaction mixture of at least an equimolar amount of a compound of the formula wherein R4 represents lower alkyl and preferably methyl, R5 represents hydrogen or lower alkyl and preferably methyl, R6 represents lower alkoxy and preferably methoxy and R7 represents lower alkoxy and preferably methoxy, previously prepared from the corresponding Dane salt and an acid chloride under anhydrous conditions in the presence of a tertiary amine as catalyst, such as N-methylmorpholine in a dry, inert, water insoluble, organo solvent such as methylene chloride mixed with a cosolvent or methyl isobutylketone or tetrahydrofuran optionally mixed with a cosolvent, and the continuation of the reactior at a temperature of -10°C or lower and preferably from 2°C to 30°C whereafter the desired compound is recovered by usual methods.

  制备含有青霉素和头孢菌素衍生物的/ D-a-氨基-对羟基-苯基乙酰胺/基团的工艺，包括式中化合物的酰化： 和/或 或 和/或 其中 R1、R2 和 R3 代表相同或不同的基团，可选自低级烷基、苄基、环烷基或苯基，优选低级烷基，更优选甲基，其中 X 代表选自氢、乙酰氧基或五元杂环硫基残基组成的组的残基，五元杂环硫基残基含有选自氮、氧和/或硫的杂原子，可选择被低级烷基取代，其中最终存在的-NH-基可选择被硅烷化、该化合物的制备方法是：将 6-氨基青霉烷酸或 7-氨基头孢烷酸或其 3-甲基修饰物与至少一个当量，就 6-APA、7-ACA 或 7-ADCA 而言最好是约 2 个当量，就 7-ACA 的其他 3-甲基修饰物而言最好是约 3 个当量的三(低级)烷基硅烷基供给剂在干燥的惰性不溶于水的溶剂中反应、将式 I-IV 化合物的预冷溶液与至少等摩尔量的式 I-IV 化合物的预冷反应混合物快速混合，制得三(低级)烷基硅烷基团供给剂的约 3 个当量的 7-ACA 其中 R4 代表低级烷基，最好是甲基；R5 代表氢或低级烷基，最好是甲基；R6 代表低级烷氧基，最好是甲氧基；R7 代表低级烷氧基，最好是甲氧基、在干燥、惰性、不溶于水的有机溶剂如二氯甲烷与助溶剂或甲基异丁基酮或四氢呋喃（任选与助溶剂混合）中，如 N-甲基吗啉，在-10℃或更低温度下，最好在 2℃至 30℃下继续反应，然后用通常的方法回收所需的化合物。
• Process and intermediates for preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate
  申请人：PFIZER INC.

  公开号：EP0108545A1

  公开（公告）日：1984-05-16

  A process for the preparation of 1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate which comprises reacting 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillante or the corresponding phenoxy- acetamidopenicillanate under anhydrous conditions with a halogenating agent in the presence of a reaction inert solvent to form an intermediate imino halide, addition of a primary alcohol having from one to four carbon atoms to convert the imino halide to an imino ether and subsequent hydrolysis to give the desired product.

  1,1-dioxopenicillanoyloxymethyl 6-beta-aminopenicillanate 的制备工艺，包括 1,1-dioxopenicillanoyloxymethyl 6-phenylacetamidopenicillante 或相应的 phenoxy- acetamidopenicillanate 在无水条件下，在反应惰性溶剂存在下与卤化剂反应，形成中间亚氨基卤化物、加入具有一至四个碳原子的伯醇，将亚胺卤化物转化为亚胺醚，然后水解得到所需的产品。
• ASCHER, G.;RIEDL, K.
  作者：ASCHER, G.、RIEDL, K.

  DOI：——

  日期：——
• Process for the preparation of a (D-alpha-amino-(p-hydroxyphenyl)-acetamido) group containing cephalosporanic acid derivatives
  申请人：GIST-BROCADES N.V.

  公开号：EP0019345B1

  公开（公告）日：1985-06-19