CAS: 151982-51-3; 4-Bromo-2-Fluorobenzoyl Chloride

相似化合物

1020718-20-0 393-52-2 57848-46-1

上下游产品

CAS号112704-79-7 4-溴-2-氟苯甲酸 | CAS号57848-46-1 4-溴-2-氟苯甲醛 | CAS号915087-33-1 恩杂鲁胺 | CAS号869569-77-7 2-溴-1-(4-溴-2-氟苯基)乙酮 | CAS号749927-69-3 N-甲基-4-溴-2-氟-苯甲酰胺 | CAS号749927-80-8 4-溴-2-氟-N,N-二甲基苯甲酰胺 | CAS号1332524-01-2 N-[3-氟-4-[(甲基氨基... | CAS号1289942-66-0 N-(3-氟-4-((甲基氨基... | CAS号114897-92-6 4-溴-2-氟苯乙酸 | CAS号179232-29-2 4-溴-2-氟苯甲酸甲酯 | CAS号889858-12-2 4-溴-2-氟苯甲酸叔丁酯

4-溴-2-氟苯甲醛置于sodium Chlorite,Sodium Dihydrogenphosphate,草酰氯,双氧水,N,N-二甲基甲酰胺体系中,用 二氯甲烷,水,乙腈 用作溶剂,化学反应 1.0H,反应生成4-溴-2-氟苯甲酰氯
参考文献:Novel 5α-Reductase Inhibitors: Synthesis,Structure−activity Studies,And Pharmacokinetic Profile Of Phenoxybenzoylphenyl Acetic Acids
标题:Novel 5α-Reductase Inhibitors: Synthesis,Structure−activity Studies,And Pharmacokinetic Profile Of Phenoxybenzoylphenyl Acetic Acids
摘要:Novel Substituted Benzoyl Benzoic Acids And Phenylacetic Acids 1-14 Have Been Synthesized And Evaluated For Inhibition Of Rat And Human Steroid 5 Alpha-Reductase Isozymes I And 2. The Compounds Turned Out To Be Potent And Selective Human Type 2 Enzyme Inhibitors,Exhibiting Ic50 Values In The Nanomolar Range. The Phenylacetic Acid Derivatives Were More Potent Than The Analogous Benzoic Acids. Bromination In The 4-Position Of The Phenoxy Moiety Led To The Strongest Inhibitor In This Class (12; Ic50 = 5 Nm),Which Was Equipotent To Finasteride. Since Oral Absorption Is Essential For A Potential Drug,12 Was Further Examined. In The Parallel Artificial Membrane Permeation Assay (Pampa) It Turned Out To Be A Good Permeator,Whereas It Was A Medium Permeator In Caco2 Cells. After Oral Administration (40 Mg/kg) To Rats A High Bioavailability And A Biological Half-Life Of 5.5 H Were Observed,Making It A Promising Candidate For Clinical Evaluation.
Doi:10.1021/jm050728W

专利信息

专利号:US-10995078-B2
优先权日:2013-03-13
标 题:Compounds and compositions for inhibition of FASN
发明人：BAIR KENNETH W; LANCIA JR DAVID R; LI HONGBIN; LOCH JAMES; LU WEI; MARTIN MATTHEW W; MILLAN DAVID S; SCHILLER SHAWN E R; TEBBE MARK J
权利人:FORMA THERAPEUTICS INC
摘要:The present invention relates to compounds and composition for inhibition of FASN, their synthesis, applications, and antidotes. An illustrative compound of the invention is shown below:

专利号:ES-2408932-T3
优先权日:2008-06-25
标 题:Synthesis and use of heterocyclic antibacterial agents

专利号:CA-2728210-A1
优先权日:2008-06-25
标 题:Synthesis and use of heterocyclic antibacterial agents

专利号:JP-2011525927-A
优先权日:2008-06-25
标 题 :Synthesis and use of heterocyclic antibacterial agents

专利号:EP-2307365-B1
优先权日:2008-06-25
标题 :Synthesis and use of heterocyclic antibacterial agents
发明人：REDDY PANDURANGA ADULLA P; MANSOOR UMAR FARUK; SIDDIQUI M ARSHAD
权利人:MERCK SHARP & DOHME

专利号:EP-2307365-A1
优先权日:2008-06-25
标 题 :Synthesis and use of heterocyclic antibacterial agents