CAS: 53531-69-4; (4-Bromophenyl)Methanesulfonyl Chloride

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1-bromomethyl-4-bromobenzene p-bromobenzyl chloride 8H9BrN2S*ClHC8H9BrN2S*ClH thioacetic acid S-(4-bromo-benzyl)ester 4-Bromphenylmethansulfonhydrazid N,N-bis(2,4-dimethoxybenzyl)-1-(4-bromophenyl)methanesulfonamide 1-(4-bromophenyl)methanesulfonamide 1-(4-bromophenyl)-N-methylmethanesulfonamide

对溴溴苄置于盐酸,N-氯代丁二酰亚胺,水体系中,用 乙醇,乙腈 作为反应溶剂,化学反应 2.0H,反应生成 对溴苄磺酰氯
参考文献:发现口服生物可利用的酞嗪酮类似物作为 Enpp1 抑制剂,用于 Sting 介导的癌症免疫治疗
标题:发现口服生物可利用的酞嗪酮类似物作为 Enpp1 抑制剂,用于 Sting 介导的癌症免疫治疗
摘要:T 细胞发炎的肿瘤微环境的缺乏限制了免疫检查点抑制剂 (Icis) 的功效.激活干扰素基因刺激物(sting)介导的先天免疫已成为癌症治疗中的一种新型治疗方法. 2',3'-Cyclic Gmp-amp (Cgamp) 是一种天然的 Sting 激动剂;然而,Cgamp 会被外核苷酸焦磷酸酶磷酸二酯酶 1 (Enpp1) 内源性降解.为了提高ici缓解率,我们开发了29F,一种以酞嗪-1(2 H)-One为核心支架的新型enpp1抑制剂. 29F在体外抑制 Enpp1 引起的 Cgamp 水解 (Ic 50 = 68 Nm),并增强免疫细胞和肿瘤细胞中 Sting 介导的 I 型干扰素反应. 29F表现出优异的代谢稳定性和生物利用度(F = 65%).口服29F在 Ct26 同基因模型中促进肿瘤生长抑制,并增加抗 Pd-L1 反应.此外,29F诱导的免疫记忆可防止肿瘤再攻击时复发,表明29F具有非常好的治疗潜力.
DOI:10.1021/acs.Jmedchem.3C01061

专利信息

专利号:US-3943157-A
优先权日:1971-07-26
标题 :Synthesis of codling moth attractant
发明人：HENRICK CLIVE A; SIDDALL JOHN B
权利人:ZOECON CORP
摘要:Sterospecific synthesis of an attractant for the codling moth by reacting sorbic aldehyde with an organo-metallic reagent to yield a 1-ether of trans-8-trans-10-dodecadiene-1,7-diol which is reduced via a 7-sulfonic acid ester to yield an ether of trans-8-trans-10-dodecadiene-1-ol and hydrolyzed to trans-8-trans-10-dodecadien-1-ol. ##SPC1##

专利号:US-3818049-A
优先权日:1971-07-26
标题:Synthesis of codling moth attractant
发明人：HENRICK C; SIDDALL J
权利人:ZOECON CORP
摘要:Sterospecific synthesis of an attractant for the codling moth by reacting sorbic aldehyde with an organo-metallic reagent to yield an 1-ether of trans-8-trans-10-dodecadiene-1.7-diol which is reduced via a 7-sulfonic acid ester to yield an ether of trans-8trans-10-dodecadiene-1-ol and hydrolyzed to trans-8-trans-10dodecadien-1-ol.

专利号:US-3856866-A
优先权日:1971-08-20
标题 :Synthesis of codling moth attactant
发明人：HENRICK C; SIDDALL J
权利人:ZOECON CORP
摘要:Stereospecific synthesis of an attractant for the codling moth by reacting a lithium salt of sorbic acid with 6-lithium hexan-1ether to yield a trans-8-trans-10-dodecadien-7-one-1-ether which is reduced to yield a trans-8-trans-10-dodecadien-7-ol-1-ether which in turn is reduced via a 7-sulfonic acid ester to yield a trans-8-trans-10-dodecadien-1-ether and hydrolyzed to trans-8trans-10-dodecadien-1-ol.

专利号:US-4222937-A
优先权日:1978-06-29
标题:Total synthesis of the utero-evacuant substance D,L-zoapatanol
发明人：CHEN ROBERT H K
权利人:ORTHO PHARMA CORP
摘要:A method of synthesizing 2S*, 3R*-6E-(2-hydroxyethylidene)-2-methyl-2-(4,8-dimethyl-5-oxo-7-nonenyl)-oxepan-3-ol, one of the active ingredients in the zoapatle plant, is described. The natural product is useful as a utero-evacuant agent.

专利号:US-4177194-A
优先权日:1978-06-29
标题 :Total synthesis of the utero-evacuant substance D,L-zoapatanol

专利号:CA-1179358-A
优先权日:1978-06-29
标题 :Total synthesis of the utero-evacuant substance d,l- zoapatanol