3,4-difluorophenyllithium | 164737-48-8

• 分子结构分类: 有机化合物 - 有机卤素化合物 - 乙烯基卤化物
• 英文名称: 3,4-difluorophenyllithium
• CAS: 164737-48-8
• 化学式: C₆H₃F₂Li
• 分子量: 120.028
• InChiKey: BYJMGRMEODCNLZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.69
• 重原子数：
  9
• 可旋转键数：
  0
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  3,4-difluorophenyllithium 、 (3R)-3-[(甲氧基甲基氨基)羰基]-1-哌啶羧酸 1,1-二甲基乙酯 以 四氢呋喃 为溶剂， 反应 2.0h， 生成 tert-butyl (R)-3-(3,4-difluorobenzoyl)piperidine-1-carboxylate
  参考文献：
  名称：

  Optimization of orally bioavailable alkyl amine renin inhibitors

  摘要：

  Structure-guided drug design led to new alkylamine renin inhibitors with improved in vitro and in vivo potency. Lead compound 21a, has an IC50 of 0.83 nM for the inhibition of human renin in plasma (PRA). Oral administration of 21a at 10 mg/kg resulted in >20 h reduction of blood pressure in a double transgenic rat model of hypertension. (C) 2009 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.bmcl.2009.11.066

文献信息

• Substituted anilinic piperidines as MCH selective antagonists
  申请人：Synaptic Pharmaceutical Corporation

  公开号：US06727264B1

  公开（公告）日：2004-04-27

  This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therepeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.

  这项发明涉及对黑素集中激素-1（MCH1）受体具有选择性的拮抗剂化合物。发明提供了一种药物组合物，包括治疗有效量的本发明化合物和药用可接受载体。本发明还提供了一种通过结合本发明的治疗有效量的化合物和药用可接受载体来制造的药物组合物。本发明进一步提供了一种制造药物组合物的方法，包括结合治疗有效量的本发明化合物和药用可接受载体。
• DNA encoding a human melanin concentrating hormone receptor (MCH1) and uses thereof
  申请人：——

  公开号：US20030082623A1

  公开（公告）日：2003-05-01

  This invention provides an isolated nucleic acid encoding a human MCH1 receptor, a purified human MCH1 receptor, vectors comprising isolated nucleic acid encoding a human MCH1 receptor, cells comprising such vectors, antibodies directed to a human MCH1 receptor, nucleic acid probes useful for detecting nucleic acid encoding human MCH1 receptors, antisense oligonucleotides complementary to unique sequences of nucleic acid encoding human MCH1 receptors, transgenic, nonhuman animals which express DNA encoding a normal or mutant human MCH1 receptor, methods of isolating a human MCH1 receptor, methods of treating an abnormality that is linked to the activity of a human MCH1 receptor, as well as methods of determining binding of compounds to mammalian MCH1 receptors. This invention provides a method of modifying the feeding behavior of a subject which comprises administering to the subject an amount of an MCH1 antagonist effective to decrease the body mass of the subject and/or decrease the consumption of food by the subject. This invention further provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject an amount of an MCH1 antagonist effective to treat the subject's depression and/or anxiety.

  这项发明提供了编码人类MCH1受体的孤立核酸，纯化的人类MCH1受体，包括编码人类MCH1受体的孤立核酸的载体，包含这种载体的细胞，针对人类MCH1受体的抗体，用于检测编码人类MCH1受体的核酸探针，互补于编码人类MCH1受体独特序列的反义寡核苷酸，表达编码正常或突变人类MCH1受体的转基因非人类动物，孤立人类MCH1受体的分离方法，治疗与人类MCH1受体活性相关的异常的方法，以及确定化合物与哺乳动物MCH1受体结合的方法。这项发明提供了一种修改受试者摄食行为的方法，包括向受试者投与足以减少受试者体重和/或减少受试者食物摄入量的MCH1拮抗剂的量。这项发明还提供了一种治疗患有抑郁和/或焦虑的受试者的方法，包括向受试者投与足以治疗受试者抑郁和/或焦虑的MCH1拮抗剂的量。
• Process for preparing sil acyclohexane-based liquid crystal compounds from silacyclohexanone compounds
  申请人：SHIN-ETSU CHEMICAL CO., LTD.

  公开号：EP0765880A1

  公开（公告）日：1997-04-02

  Silacyclohexane-based liquid crystal compounds are prepared from a cyclohexanone compound of the following general formula (I) wherein Ar represents a phenyl group or a tolyl group, and R represents a phenyl group, a tolyl group, a linear alkyl group having from 1 to 10 carbon atoms, a mono or difluoroalkyl group having from 1 to 10 carbon atoms, a branched alkyl group having from 3 to 8 carbon atoms or an alkoxyalkyl group having from 2 to 7 carbon atoms, and also from organolithium reagents, followed by hydrogenolysis or hydrogenation after dehydration, with or without further reaction with organometal reagents, and then to de-silylation and reduction.

  基于硅环己烷的液晶化合物是从以下通用式(I)的环己酮化合物制备而成，其中Ar代表苯基或甲苯基，R代表苯基、甲苯基、具有1至10个碳原子的直链烷基、具有1至10个碳原子的单氟或二氟烷基、具有3至8个碳原子的支链烷基或具有2至7个碳原子的烷氧基烷基，然后从有机锂试剂制备，随后脱水后进行氢解或氢化，可以选择进一步与有机金属试剂反应，然后进行脱硅和还原。
• DNA ENCODING A HUMAN MELANIN CONCENTRATING HORMONE RECEPTOR (MCH1) AND USES THEREOF
  申请人：Synaptic Pharmaceutical Corporation

  公开号：EP1246847A2

  公开（公告）日：2002-10-09
• US6727264B1
  申请人：——

  公开号：US6727264B1

  公开（公告）日：2004-04-27