2-氨基-1-(2,4-二氯苯基)乙酮盐酸盐 | 65146-54-5

• 物质功能分类: 有机原料 - 羧酸类化合物及衍生物
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 2-氨基-1-(2,4-二氯苯基)乙酮盐酸盐
• 中文别名: 2-氨基-2',4'-二氯苯乙酮盐酸盐
• 英文名称: 2-amino-1-(2,4-dichlorophenyl)ethanone hydrochloride
• 英文别名: 2-amino-1-(2,4-dichlorophenyl)ethanone;hydrochloride
• CAS: 65146-54-5
• 化学式: C₈H₇Cl₂NO*ClH
• 分子量: 240.517
• InChiKey: RJCPEUKXHFGBSW-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.56
• 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：
  43.1
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为产物：
  描述：

  (R)-N-tert-butanesulfinyl 2-(2,4-dichlorophenyl)-2oxoethylamine 在 盐酸 作用下， 以 甲醇 为溶剂， 反应 1.0h， 以86%的产率得到2-氨基-1-(2,4-二氯苯基)乙酮盐酸盐
  参考文献：
  名称：

  重排ñ -叔-Butanesulfinylα-晕与醇盐亚胺到ñ -叔-Butanesulfinyl 2-氨基缩醛作为的前体ñ和-protected Ñ -Unprotectedα氨基羰基化合物

  摘要：

  的反应ñ -叔-butanesulfinylα卤代亚胺与得到新的醇盐ñ -叔-butanesulfinyl 2-氨基缩醛以良好至优异的产量。这些ñ -叔-butanesulfinyl 2-氨基缩醛是用于相应的将TMSOTf促进的合成前体的便利ñ -保护的α氨基醛和酮，以及为2-氨基乙缩醛盐酸盐和α-盐酸促进的合成氨基酮和α-氨基醛盐酸盐的收率高。通过这种方法，实现了（S）-卡西酮盐酸盐的非对称合成（er 94：6）。

  DOI：

  10.1021/jo300752c

文献信息

• Heterocyclic carboxamide derivatives as inhibitors of nitric oxide production
  申请人：Fujisawa Pharmaceutical Co. Ltd.

  公开号：US20020132809A1

  公开（公告）日：2002-09-19

  1 wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases such as adult respiratory distress syndrome, cardiovascular ischemia, myocarditis, heart failure, synovitis, shock, diabetes, diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, glomerulonephritis, peptic ulcer, inflammatory bowel disease, cerebral infarction, cerebral ischemia, cerebral hemorrhage, migraine, rheumatoid arthritis, gout, neuritis, postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, metastasis, Alzheimer's disease, arthritis, CNS disorders, dermatitis, hepatitis, liver cirrhosis, multiple sclerosis, pancreatitis, atherosclerosis, and the like in human being and animals.

  本发明的化合物(I)及其药学上可接受的盐，其中每个符号如规范所定义。该化合物(I)及其药学上可接受的盐对一氧化氮(NO)的生成具有强烈的抑制活性，适用于预防和/或治疗NO介导的疾病，例如成人呼吸窘迫综合征、心血管缺血、心肌炎、心力衰竭、滑膜炎、休克、糖尿病、糖尿病肾病、糖尿病视网膜病变、糖尿病神经病变、肾小球肾炎、消化性溃疡、炎症性肠病、脑梗塞、脑缺血、脑出血、偏头痛、类风湿性关节炎、痛风、神经炎、带状疱疹后神经痛、骨关节炎、骨质疏松症、系统性红斑狼疮、器官移植排斥、哮喘、转移、阿尔茨海默病、关节炎、中枢神经系统疾病、皮炎、肝炎、肝硬化、多发性硬化症、胰腺炎、动脉粥样硬化等人类和动物中的疾病。
• HETEROCYCLIC CARBOXAMIDE DERIVATIVES AS INHIBITORS OF NITRIC OXIDE PRODUCTION
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：EP1075475A1

  公开（公告）日：2001-02-14
• [EN] HETEROCYCLIC CARBOXAMIDE DERIVATIVES AS INHIBITORS OF NITRIC OXIDE PRODUCTION<br/>[FR] DERIVES DE CARBOXAMIDE HETEROCYCLIQUES UTILISEES COMME INHIBITEURS DE LA PRODUCTION DE MONOXYDE D'AZOTE
  申请人：FUJISAWA PHARMACEUTICAL CO., LTD.

  公开号：WO1999057114A1

  公开（公告）日：1999-11-11

  (EN) A compound of formula (I), wherein each symbol is as defined in the specification, and pharmaceutically acceptable salts thereof. The compound (I) of the present invention and pharmaceutically acceptable salts thereof possess a strong inhibitory activity on the production of nitric oxide (NO), and are useful for prevention and/or treatment of NO-mediated diseases such as adult respiratory distress syndrome, cardiovascular ischemia, myocarditis, heart failure, synovitis, shock, diabetes, diabetic nephropathy, diabetic retinopathy, diabetic neuropathy, glomerulonephritis, peptic ulcer, inflammatory bowel disease, cerebral infarction, cerebral ischemia, cerebral hemorrhage, migraine, rheumatoid arthritis, gout, neuritis, postherpetic neuralgia, osteoarthritis, osteoporosis, systemic lupus erythematosus, rejection by organ transplantation, asthma, metastasis, Alzheimer's disease, arthritis, CNS disorders, dermatitis, hepatitis, liver cirrhosis, multiple sclerosis, pancreatitis, atherosclerosis, and the like in human being and animals.(FR) L'invention porte sur un composé de la formule (I) dans laquelle chaque symbole est tel que défini dans la demande, et sur les sels pharmaceutiquement acceptables de celui-ci. Le composé (I) de cette invention et ses sels pharmaceutiquement acceptables ont une forte activité inhibitrice sur la production de monoxyde d'azote (NO), et sont utiles dans la prévention et/ou le traitement de maladies induites par NO telles que l'insuffisance respiratoire aiguë des états de choc, l'ischémie cardio-vasculaire, la myocardite, l'insuffisance cardiaque, la synovite, l'état de choc, les diabètes, la néphropathie diabétique, la rétinopathie diabétique, la neuropathie diabétique, la glomérulonéphrite, l'ulcère gastro-duodénal, les maladies intestinales inflammatoires, l'infarctus cérébral, l'ischémie cérébrale, l'hémorragie cérébrale, la migraine, l'arthrite rhumatoïde, la goutte, la névrite, l'algie post-zostérienne, l'arthrose, l'ostéoporose, le lupus érythémateux disséminé, le rejet après transplantation d'organe, l'asthme, la métastase, la maladie d'Alzheimer, l'arthrite, les troubles du système nerveux central, les dermatites, l'hépatite, la cirrhose du foie, la sclérose en plaques, la pancréatite, l'athérosclérose et autre, chez l'homme et l'animal.
• Rearrangement of <i>N</i>-<i>tert</i>-Butanesulfinyl α-Halo Imines with Alkoxides to <i>N</i>-<i>tert</i>-Butanesulfinyl 2-Amino Acetals as Precursors of <i>N</i>-Protected and <i>N</i>-Unprotected α-Amino Carbonyl Compounds
  作者：Filip Colpaert、Sven Mangelinckx、Bram Denolf、Norbert De Kimpe

  DOI：10.1021/jo300752c

  日期：2012.7.20

  imines with alkoxides afforded new N-tert-butanesulfinyl 2-amino acetals in good to excellent yield. These N-tert-butanesulfinyl 2-amino acetals are convenient precursors for the TMSOTf-promoted synthesis of the corresponding N-protected α-amino aldehydes and ketones, as well as for the HCl-promoted synthesis of 2-amino acetal hydrochlorides and α-amino ketone and α-amino aldehyde hydrochlorides in high

  的反应ñ -叔-butanesulfinylα卤代亚胺与得到新的醇盐ñ -叔-butanesulfinyl 2-氨基缩醛以良好至优异的产量。这些ñ -叔-butanesulfinyl 2-氨基缩醛是用于相应的将TMSOTf促进的合成前体的便利ñ -保护的α氨基醛和酮，以及为2-氨基乙缩醛盐酸盐和α-盐酸促进的合成氨基酮和α-氨基醛盐酸盐的收率高。通过这种方法，实现了（S）-卡西酮盐酸盐的非对称合成（er 94：6）。