CAS: 85952-30-3; (3,4-Dichlorophenyl)Methanesulfonyl Chloride

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CAS号102-47-6 3,4-二氯氯苄 | CAS号111875-15-1 sodium 3,4-dich... | CAS号904674-08-4 (3,4-二氯苯基)甲磺酰胺

📜3,4-二氯氯苄置于盐酸,N-氯代丁二酰亚胺体系中,用 乙醇,水,乙腈 作为反应溶剂,化学反应 1.5H,反应生成 (3,4-二氯苯基)甲磺酰氯
参考文献:通过铜催化的三组分反应,设计新型的基于n-磺酰胺基衍生物的c-Met抑制剂.
标题:通过铜催化的三组分反应,设计新型的基于n-磺酰胺基衍生物的c-Met抑制剂.
摘要:在我们不断努力开发新颖的c-Met抑制剂作为潜在的抗癌候选药物的过程中,设计了一系列新的n-磺酰lam啶衍生物,并通过cu催化的多组分反应(mcr)合成了关键步骤,并对它们的体外生物学活性进行了评估.抗c-Met激酶和四种癌细胞系(a549,Ht-29,Mkn-45和mda-Mb-231).大多数目标化合物在基于酶和基于细胞的测定中均显示出中等至显着的效力,并且对a549和ht-29癌细胞系具有选择性.sar的初步研究表明,化合物26Af(c-Met Ic 50 与阳性的foretinib相比,它具有2.89 Nm)的最有前途的化合物,后者具有显着的抗增殖活性,Ic 50值为0.28至0.72μm.对26Af的机理研究表明,抗癌活性与c-Met的阻断磷酸化密切相关,导致细胞周期停滞在g2 / M期,并以浓度依赖的方式导致a549细胞凋亡.有希望的化合物26Af被进一步鉴定为c-Met激酶的相对选择性抑制剂,在balb
DOI:10.1016/j.Ejmech.2020.112470

专利信息

专利号:US-7259277-B2
优先权日:2003-07-25
标题 :Advanced route for the synthesis of cPLA2 inhibitors
发明人：WU YANZHONG; RAVEENDRATH PANOLIL
权利人:WYETH CORP
摘要:A process for making a compound of formula (I) n nin which process the compound HC≡C—(CH 2 ) n —NH 2 is reacted with the compound R 1 —SO 2 Cl to produce an intermediate compound, which intermediate compound is then reacted with the compound of formulan n nto produce the compound of formula (I), and compounds produced by the process of this invention. The terms R 1 , R 2 , R 3 , R 4 and n have the definitions set forth in the specification.

专利号:US-7582771-B2
优先权日:2003-09-03
标题:Process for the synthesis of cPLA2 inhibitors
发明人：DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL; REN JIANXIN; WU CHARLES C; WU YANGZHONG
权利人:WYETH CORP
摘要:A process for making the compound of formula (I) n nwherein Ac represents acetate; X represents O or CH 2 ; Y represents C 1 -C 6 alkyl; and Z is selected from the group consisting of H, halogen, CN, CHO, CF 3 , OCF 3 , OH, C 1 -C 6 alkyl, C 1 -C 6 alkoxy, C 1 -C 6 thioalkyl, NH 2 , N(C 1 -C 6 alkyl) 2 , NH(C 1 -C 6 alkyl), NC(O)—(C 1 C 6 alkyl), and NO 2 . In his process, a compound of formula (II)n n nis reacted with hydrazine to form a primary alkylamine, and then the primary alkylamine is reacted with acetic anhydride, to produce the compound of formula (I).

专利号:US-7342119-B2
优先权日:2003-09-30
标题 :Process for the synthesis of a CPLA2 inhibitor
发明人：DEHNHARDT CHRISTOPH M; MEGATI SREENIVASULU; MICHALAK RONALD S; RAVEENDRANATH PANOLIL
权利人:WYETH CORP
摘要:A process for making a substituted indole compound, including the steps of: reacting the compounds n nin a non-protic polar solvent in the presence of a catalyst to form the intermediate compoundn n nwherein Ph and X are as defined herein; and then,n nheating this intermediate compound in the solvent in the presence of the catalyst to form the substituted indole compoundn n nThe invention also includes compounds formed by this process.

专利号:US-2005049296-A1
优先权日:2003-09-03
标 题 :Process for the synthesis of cPLA2 inhibitors

专利号:US-2008177085-A1
优先权日:2003-09-30
标 题:Process for the Synthesis of a CPLA2 Inhibitor

专利号:US-2005070723-A1
优先权日:2003-09-30
标 题 :Process for the synthesis of a CPLA2 inhibitor