CAS: 456-06-4; 4-Fluorobenzohydrazide

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CAS号451-46-7 4-氟苯甲酸乙酯 | CAS号403-33-8 对氟苯甲酸甲酯 | CAS号456-22-4 对氟苯甲酸 | CAS号2714-90-1 4-fluorobenzoic... | CAS号403-43-0 对氟苯甲酰氯 | CAS号141079-02-9 3-(4-fluorophen... | CAS号141078-94-6 4H-1,2,4-Triazo... | CAS号41421-13-0 5-(4-氟苯基)-1,3,4... | CAS号29552-52-1 4-乙基-5-(4-氟苯基)-... | CAS号824-75-9 4-氟苯甲酰胺 | CAS号721428-34-8 5-(氯甲基)-3-(4-氟苯... | CAS号61019-25-8 4-AMINO-5-(4-FL... | CAS号1580-50-3 1,3,4-Oxadiazol... | CAS号114058-91-2 5-(4-氟苯)-4H-1,2... | CAS号138417-35-3 5-(4-氟苯基)-4-甲基-...

对氟苯甲酸置于硫酸,Hydrazine Hydrate,碳酸氢钠,溶剂黄146体系中,用 乙醇 作为反应溶剂,化学反应 6.0H,以97%的收率获得产物4-氟苯甲酰肼
参考文献:新型5-(芳酰基肼基羰基)依他普仑作为胆碱酯酶抑制剂的合成
标题:新型5-(芳酰基肼基羰基)依他普仑作为胆碱酯酶抑制剂的合成
摘要:已经设计,合成和测试了一系列新型的5-(芳酰基肼基羰基)依他普仑(58-84)对胆碱酯酶的抑制潜力.发现3-氯苯甲酰基-(71)是该系列中最有效的化合物,对乙酰胆碱酯酶(ache)的抑制作用的ic 50为1.80+/-0.11μm.对于丁酰胆碱酯酶(bche)抑制,2-溴苯甲酰基-(76)是该系列中活性最高的化合物,Ic 50为2.11+/-0.31μm.构效关系说明温和的给电子基团增强了酶的抑制作用,而吸电子基团降低了除o-No 2以外的抑制.然而,取代基的大小和位置影响酶抑制..在ache的对接研究中,配体71,72和76分别显示5874,5756和5666以及ace的得分分别为-64.92,-203.25和-140.29 Kcal / Mol.在bche的情况下,配体71,76和81分别显示出ace值为-170.91,-256.84和-235.97 Kcal / Mol的高分6016,6150和5994.
DOI:10.1016/j.Ejmech.2017.06.036

专利信息

专利号:US-8772301-B2
优先权日:2009-12-18
标题 :Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
发明人：HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D
权利人:HARDY LARRY WENDELL; HEFFERNAN MICHELE L R; WU FRANK XINHE; SPEAR KERRY L; SARASWAT LAKSHMI D; SUNOVION PHARMACEUTICALS INC
摘要:Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.

专利号:US-2019152962-A1
优先权日:2016-07-14
标题 :Cyclopropyl derivatives as ror-gamma modulators
发明人：DESAI RANJIT; KUMAR SANJAY S; PANDYA VRAJESH; DESAI JIGAR; RAVAL SAURIN
权利人:CADILA HEALTHCARE LTD
摘要:The present invention provides compounds which are modulators of RORγ and their use for the treatment of diseases or conditions mediated by RORγ. Further, the present invention relates to processes of preparing such compounds, their tautomeric forms, novel intermediates involved in their synthesis, their pharmaceutically acceptable salts, methods for using such compounds and pharmaceutical compositions containing them (Formula I).

专利号:CN-114835656-A
优先权日:2022-05-13
标 题:A kind of ethyl 1,3,4-oxadiazole acetate and its synthesis method

专利号:CN-119977833-A
优先权日:2025-01-22
标题:Synthesis and antitumor application of erianin derivative