2,4-diamino-6-quinazolinesulfonyl chloride sulfate | 92144-33-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 英文名称: 2,4-diamino-6-quinazolinesulfonyl chloride sulfate
• 英文别名: 2,4-Diamino-quinazoline-6-sulfonyl chloride sulfate salt；2,4-diaminoquinazoline-6-sulfonyl chloride;sulfuric acid
• CAS: 92144-33-7
• 化学式: C₈H₇ClN₄O₂S*H₂O₄S
• 分子量: 356.768
• InChiKey: YEIZCIHTAAWELE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0.07
• 重原子数：
  21
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  203
• 氢给体数：
  4
• 氢受体数：
  10

反应信息

• 作为反应物：
  描述：

  2,4-diamino-6-quinazolinesulfonyl chloride sulfate 在 ammonium hydroxide 作用下， 反应 1.0h， 生成 2,4-Diamino-6-sulfamoyl-chinazolin
  参考文献：
  名称：

  Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides

  摘要：

  The synthesis and antimalarial activity of a series of 2,4-diamino-6-quinazolinesulfonamides (III) is described. Chlorosulfonation of 2,4-quinazolinediamine affords the 6-sulfonyl chloride, which upon treatment with the appropriate amine produces the desired products. Alternatively the sulfonyl chloride could be introduced by diazotization of the corresponding amine followed by treatment with SO2 in the presence of CuCl2. Although substantial antimalarial activity was demonstrated for several members of this class, studies were discontinued in light of the potency of related series.

  DOI：

  10.1021/jm00378a038
• 作为产物：
  描述：

  喹唑啉-2,4-二胺硫酸盐 在 chlorosulphuric acid 、 sodium chloride 作用下， 反应 3.0h， 以99%的产率得到2,4-diamino-6-quinazolinesulfonyl chloride sulfate
  参考文献：
  名称：

  Folate antagonists. 22. Antimalarial and antibacterial effects of 2,4-diamino-6-quinazolinesulfonamides

  摘要：

  The synthesis and antimalarial activity of a series of 2,4-diamino-6-quinazolinesulfonamides (III) is described. Chlorosulfonation of 2,4-quinazolinediamine affords the 6-sulfonyl chloride, which upon treatment with the appropriate amine produces the desired products. Alternatively the sulfonyl chloride could be introduced by diazotization of the corresponding amine followed by treatment with SO2 in the presence of CuCl2. Although substantial antimalarial activity was demonstrated for several members of this class, studies were discontinued in light of the potency of related series.

  DOI：

  10.1021/jm00378a038

文献信息

• ELSLAGER, E. F.;COLBRY, N. L.;DAVOLL, J.;HUTT, M. P.;JOHNSON, J. L.;WERBE+, J. MED. CHEM., 1984, 27, N 12, 1740-1743
  作者：ELSLAGER, E. F.、COLBRY, N. L.、DAVOLL, J.、HUTT, M. P.、JOHNSON, J. L.、WERBE+

  DOI：——

  日期：——
• US05958918
  申请人：——

  公开号：——

  公开（公告）日：——
• SUBSTITUTED (SULFINIC ACID, SULFONIC ACID, SULFONYLAMINO OR SULFINYLAMINO) N- (AMINOIMINOMETHYL)PHENYLALKYL -AZAHETEROCYCLYLAMIDE COMPOUNDS
  申请人：Aventis Pharmaceuticals Inc.

  公开号：EP0853618B1

  公开（公告）日：2011-08-17
• US5958918A
  申请人：——

  公开号：US5958918A

  公开（公告）日：1999-09-28
• [EN] SUBSTITUTED (SULFINIC ACID, SULFONIC ACID, SULFONYLAMINO OR SULFINYLAMINO) N-[(AMINOIMINOMETHYL)PHENYLALKYL]-AZAHETEROCYCLYLAMIDE COMPOUNDS<br/>[FR] COMPOSES D'(ACIDE SULFINIQUE, ACIDE SULFONIQUE, SULFONYLAMINO OU SULFINYLAMINO) N-[(AMINOIMINOMETHYL)PHENYLALKYL]-AZAHETEROCYCLYLAMIDE SUBSTITUES
  申请人：RHÔNE-POULENC RORER PHARMACEUTICALS INC.

  公开号：WO1996040679A1

  公开（公告）日：1996-12-19

  (EN) The compounds of formula (I) exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More especially, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula (I), compositions containing compounds of formula (I), and their use, which are for treating a patient suffering from, or subject to, physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.(FR) Les composés de formule (I) présentent une utilité pharmacologique et, de ce fait, on les incorpore dans des compositions pharmaceutiques et on les utilise dans le traitement de patients souffrant de certains troubles médicaux. Ils sont, plus particulièrement, des inhibiteurs de l'activité du Facteur Xa. L'invention concerne des composés de formule (I), des compositions contenant lesdits composés, ainsi que leur utilisation dans le traitement de patients souffrant d'états physiologiques, ou sujets à ces états, qu'on peut améliorer par administration d'un inhibiteur de l'activité du Facteur Xa.