CAS: 186589-76-4; 5-Chloro-2-Fluorophenol

5-氯-2-氟苯胺置于硫酸,Sodium Nitrite,Copper(II) Sulfate体系中,用 水 用作溶剂,化学反应 2.5H,以40%的收率获得5-氯-2-氟苯酚
参考文献: Non-Nucleotide Reverse Transcriptase Inhibitors[fr] Inhibiteurs De La Transcriptase Inverse Non Nucleosidiques
标题: Non-Nucleotide Reverse Transcriptase Inhibitors[fr] Inhibiteurs De La Transcriptase Inverse Non Nucleosidiques
摘要:化合物的公式z:其中;A为ch或n;R1是一个取代基,连接到包含a的环中的一个碳原子,所选自-S(=o)Pra,其中ra为-C1-C4烷基,-Orx,-Nrxrx,-Nhnrxrx,-Nhnhc(=o)Orx,-Nrxoh;-C(=o)-Rb,其中rb为-Ct-C4-烷基,Orx,-Nrxrx,-Nhnrxrx,-Nhc1-C3-烷基-C(=o)Orx-Nrxrc,其中rc为h,C1-C4烷基,-Nrxrx;-C(=0)Rd,-Cn,S(=o)Prx,其中rd为c1-C4-烷基,-Orx,-Nrxrx C1-C3-烷基-O-Cl-C3烷基c(=o)Orx,-C1-C3-烷基-Coorx;-C1-C3烷基-Oh或c1-C4烷基的醚或酯(o-Cl-C3烷基)q-O-Rx,一个含有1-3个杂原子的5或6元芳香环,P为1或2;Rx独立选择自h,C1-C4烷基或乙酰基;或一对rx可以与相邻的n原子一起形成环;L为-0-,-S(=o),-或-Ch2-,其中r为0,1或2;R3-R7为规范中定义的取代基;X为-(Cr8R8')N-D-(Cr8R8')M-;D为键,-Nr9-,-0-,-S-,-S(=0)-或-S(=0)2-;以及其药学上可接受的盐和前药,具有作为hiv抗病毒药物的用途.

专利信息

专利号:US-6828466-B2
优先权日:2002-07-19
标题:Process for the synthesis of phenols from arenes
发明人：MALECZKA JR ROBERT E; SMITH III MILTON R; HOLMES DANIEL; SHI FENG
权利人:UNIV MICHIGAN STATE
摘要:A process to synthesize substituted phenols such as those of the general formula RR'R''Ar(OH) wherein R, R', and R'' are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C-H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.

专利号:US-7405310-B2
优先权日:2001-03-05
标 题:Non-nucleoside reverse transcriptase inhibitors
发明人：LINDSTROM STEFAN; SAHLBERG CHRISTER; WALLBERG HANS; KALYANOV GENAIDY; ODEN LOURDES SALVADOR; NAESLUND LOTTA
权利人:MEDIVIR AB
摘要:This invention relates to non-nucleoside reverse transcriptase inhibitors active against HIV-1 and having an improved resistance and pharmacokinetic profile. The invention further relates to novel intermediates in the synthesis of such compounds and the use of the compounds in antiviral methods and compositions.

专利号:US-2004030197-A1
优先权日:2002-07-19
标 题 :Process for the synthesis of phenols from arenes

专利号:CN-109134204-A
优先权日:2018-11-16
标 题:Synthesis of intermediate 2-bromo-4-fluoro-5-chlorophenol