5-甲基-2-苯基-噁唑-4-甲酰氯 | 51655-71-1

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑类
• 中文名称: 5-甲基-2-苯基-噁唑-4-甲酰氯
• 中文别名: 5-甲基-2-苯基-1,3-恶唑-4-甲酰氯
• 英文名称: 2-phenyl-5-methyl-4-oxazolecarboxylic acid chloride
• 英文别名: 5-methyl-2-phenyl-oxazole-4-carbonyl chloride；5-Methyl-2-phenyl-oxazol-4-carbonylchlorid；5-methyl-2-phenyl-4-oxazolecarboxylic acid chloride；2-phenyl-5-methyl-oxazole-4-carboxyl chloride；5-Methyl-2-phenyl-1,3-oxazole-4-carbonyl chloride
• CAS: 51655-71-1
• 化学式: C₁₁H₈ClNO₂
• mdl: MFCD08271880
• 分子量: 221.643
• InChiKey: RWVAPUPMWDZLGV-UHFFFAOYSA-N

物化性质

• 熔点：
  135 °C

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.09
• 拓扑面积：
  43.1
• 氢给体数：
  0
• 氢受体数：
  3

安全信息

• 海关编码：
  2934999090

反应信息

• 作为反应物：
  描述：

  5-甲基-2-苯基-噁唑-4-甲酰氯 在 Pd-BaSO₄ 、 xylene 作用下， 生成 5-甲基-2-苯基-1,3-噁唑-4-甲醛
  参考文献：
  名称：

  192.恶唑-4-羧酸的一些反应

  摘要：

  DOI：

  10.1039/jr9520001085
• 作为产物：
  描述：

  1-(5-甲基-2-苯基-1,3-恶唑-4-基)乙酮 在 磺酰氯 、 sodium hypobromide 作用下， 以 1,4-二氧六环 、 N,N-二甲基甲酰胺 为溶剂， 生成 5-甲基-2-苯基-噁唑-4-甲酰氯
  参考文献：
  名称：

  Photochemical transformations of small ring heterocyclic compounds. 70. Thermal and photochemical valence isomerizations of 4-carbonyl-substituted isoxazoles

  摘要：

  DOI：

  10.1021/ja00855a033

文献信息

• [EN] INDOLE AMIDE DERIVATIVES AND RELATED COMPOUNDS FOR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES<br/>[FR] DÉRIVÉS D'INDOLAMIDE ET COMPOSÉS ASSOCIÉS DESTINÉS À ÊTRE UTILISÉS DANS LE TRAITEMENT DES MALADIES NEURODÉGÉNÉRATIVES
  申请人：UNIV LEUVEN KATH

  公开号：WO2010142801A1

  公开（公告）日：2010-12-16

  This invention provides novel compounds and the novel compounds for use as a medicine, more in particular for the prevention or treatment of neurodegenerative disorders, more specifically certain neurological disorders, such as disorders collectively known as tauopathies, and disorders characterised by cytotoxic α-synuclein amyloidogenesis. The present invention also relates to the use of said novel compounds for the manufacture of medicaments useful for treating such neurodegenerative disorders. The present invention further relates to pharmaceutical compositions including said novel compounds and to methods for the preparation of said novel compounds.

  本发明提供了新型化合物，以及这些新型化合物作为药物的使用，特别是用于预防或治疗神经退行性疾病，更具体地是一些神经系统疾病，例如统称为tauopathies的疾病，以及以细胞毒性α-突触核蛋白淀粉样蛋白生成为特征的疾病。本发明还涉及将所述新型化合物用于制造用于治疗此类神经退行性疾病的药物。本发明还涉及包括所述新型化合物的药物组合物，以及制备所述新型化合物的方法。
• [EN] INHIBITORS OF DIACYLGLYCEROL ACYL TRANSFERASE<br/>[FR] INHIBITEUR DE DIACYLGLYCÉROL ACYLTRANSFÉRASE
  申请人：PIRAMAL LIFE SCIENCES LTD

  公开号：WO2011080718A1

  公开（公告）日：2011-07-07

  The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.

  本发明涉及杂环化合物及其所有立体异构体和互变异构体形式；以及它们的药学上可接受的盐、药学上可接受的溶剂合物和药学上可接受的多晶形态。该发明还涉及制备这些杂环化合物的方法以及含有它们的药物组合物。所述化合物及其药物组合物在预防和治疗由二酰基甘油酰基转移酶（DGAT）介导的疾病或紊乱方面具有用途，特别是DGAT1。本发明进一步提供了一种治疗这些疾病或紊乱的方法，通过向有需要的哺乳动物施用所述化合物或其药物组合物的治疗有效量。
• Fluorinated lysine derivatives as dipeptidyl peptidase IV inhibitors
  申请人：Parker C. Janice

  公开号：US20050043292A1

  公开（公告）日：2005-02-24

  The invention relates to new therapeutically active and selective inhibitors of the enzyme dipeptidyl peptidase-IV (“DPP-IV”), pharmaceutical compositions comprising the compounds and the use of such compounds for treating diseases that are associated with proteins that are subject to processing by DPP-IV, such as Type 2 diabetes, metabolic syndrome (syndrome X or insulin resistance syndrome), hyperglycemia, impaired glucose tolerance, glucosuria, metabolic acidosis, arthritis, cataracts, diabetic neuropathy, diabetic nephropathy, diabetic retinopathy, diabetic cardiomyopathy, Type 1 diabetes, obesity, conditions exacerbated by obesity, hypertension, hyperlipidemia, atherosclerosis, osteoporosis, osteopenia, frailty, bone loss, bone fracture, acute coronary syndrome, infertility due to polycystic ovary syndrome, short bowel syndrome, anxiety, depression, insomnia, chronic fatigue, epilepsy, eating disorders, chronic pain, alcohol addiction, diseases associated with intestinal motility, ulcers, irritable bowel syndrome, inflammatory bowel syndrome and to prevent disease progression in Type 2 diabetes. The invention also relates to a method of identifying an insulin secretagogue agent for diabetes.

  该发明涉及新的具有治疗活性和选择性的酶二肽基肽酶-IV（“DPP-IV”）抑制剂，包括这些化合物的药物组合物以及利用这些化合物治疗与受DPP-IV加工的蛋白质相关的疾病，如2型糖尿病、代谢综合征（综合征X或胰岛素抵抗综合征）、高血糖、糖耐量受损、糖尿病、代谢性酸中毒、关节炎、白内障、糖尿病性神经病变、糖尿病性肾病、糖尿病性视网膜病变、糖尿病性心肌病、1型糖尿病、肥胖、由肥胖恶化的疾病、高血压、高脂血症、动脉粥样硬化、骨质疏松症、脆弱性、骨质流失、骨折、急性冠状动脉综合征、多囊卵巢综合征导致的不孕症、短肠综合征、焦虑、抑郁症、失眠、慢性疲劳、癫痫、进食障碍、慢性疼痛、酒精成瘾、与肠道蠕动有关的疾病、溃疡、肠易激综合征、炎症性肠病以及预防2型糖尿病疾病进展的方法。该发明还涉及一种用于识别糖尿病胰岛素分泌素的方法。
• DIACYLGLYCEROL ACYLTRANSFERASE INHIBITORS
  申请人：Bolin David Robert

  公开号：US20090076275A1

  公开（公告）日：2009-03-19

  Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity, type II diabetes mellitus and metabolic syndrome.

  本文提供了式(I)的化合物，以及其药用盐，其中取代基如规范中所披露的那样。这些化合物及含有它们的药物组合物对于治疗疾病如肥胖、II型糖尿病和代谢综合征等方面是有用的。
• Monoamino 2,4,5-trisubstituted oxazoles
  申请人：Gruppo Lepetit S.p.A.

  公开号：US04072689A1

  公开（公告）日：1978-02-07

  Pharmacologically active 2,4,5-trisubstituted oxazoles of the general formula ##STR1## wherein A is cyclohexyl, thienyl or a group of the formula ##STR2## in which R represents one to three substituents each independently selected from the group consisting of hydrogen, lower alkyl, halo, halo-lower alkyl, lower alkoxy, nitro, cyano, amino, carbamoyl, acetamino or carboxy; one of the R.sub.1 and R.sub.2 groups is a lower alkyl group and the other is an amido group, ##STR3## wherein R.sub.3 is selected from the group consisting of hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, hydroxy, amino, lower alkylideneamino, cycloalkylideneamino, benzylideneamino and R.sub.4 is selected from hydrogen, lower alkyl, lower alkenyl, cycloalkyl, phenyl, substituted phenyl, phenyl-lower alkyl, hydroxy-lower alkyl, lower acyloxy-lower alkyl, or R.sub.3 and R.sub.4 taken together with the nitrogen atom may also form a 5- to 7-membered hetero ring which may contain one other hetero atom selected from N, O and S. The compounds have antiinflammatory activity.

  药理活性的2,4,5-三取代噁唑的通式为##STR1##其中A为环己基，噻吩基或公式##STR2##的基团，其中R代表从氢，低级烷基，卤素，卤素-低级烷基，低级烷氧基，硝基，氰基，氨基，氨基甲酰基，乙酰氨基或羧基选择的一个至三个取代基，R.sub.1和R.sub.2基团中的一个是低级烷基基团，另一个是酰胺基团，##STR3##其中R.sub.3选择自氢，低级烷基，低级烯基，环烷基，苯基，取代苯基，苯基-低级烷基，羟基-低级烷基，低级酰氧基-低级烷基，羟基，氨基，低级烷基亚胺基，环烷基亚胺基，苄亚胺基和R.sub.4选择自氢，低级烷基，低级烯基，环烷基，苯基，取代苯基，苯基-低级烷基，羟基-低级烷基，低级酰氧基-低级烷基，或R.sub.3和R.sub.4与氮原子一起也可以形成一个5-至7-成员的杂环，其中可能包含另一个从N，O和S选择的杂原子。这些化合物具有抗炎活性。