CAS: 1228780-71-9; Tert-Butyl 4-((4'-Chloro-5,5-Dimethyl-3,4,5,6-Tetrahydro-[1,1'-Biphenyl]-2-yl)Methyl)Piperazine-1-Carboxylate

相似化合物

1228780-72-0 1628047-87-9 2089325-11-9

上下游产品

2-(4-氯苯基)-4,4-二甲基-1-环己烯-1-羧醛 2-(4-Chlorophenyl)-4,4-Dimethylcyclohex-1-Enecarbaldehyde 1228837-05-5
1-(2-(Bromomethyl)-5,5-Dimethylcyclohex-1-Enyl)-4-Chlorobenzene
2-(4-氯苯基)-4,4-二甲基环己-1-烯-1-羧酸甲酯 Methyl 2-(4-Chlorophenyl)-4,4-Dimethylcyclohex-1-Enecarboxylate 1228780-49-1

3,3-二甲基环己酮置于四丁基溴化铵,三乙酰氧基硼氢化钠,三氯氧磷体系中,用 四氢呋喃,二氯甲烷,N,N-二甲基甲酰胺,甲苯 用作溶剂,化学反应 26.25H,反应生成4-[[2-(4-氯苯基)-4,4-二甲基环己-1-烯基]甲基]哌嗪-1-羧酸叔丁酯
参考文献:Venetoclax(一种一流的bcl-2选择性抑制剂)的收敛大规模合成方法的开发.
标题:Venetoclax(一种一流的bcl-2选择性抑制剂)的收敛大规模合成方法的开发.
摘要:描述了一种新的合成路线的工艺开发,该路线导致了venetoclax(1:Venclexta中的活性药物成分(api))的高效,稳健的合成工艺.重新设计的合成设有buchwald-Hartwig偶联反应来构建芯酯23C通过连接两个关键构建块(以会聚方式4C和26),然后,接着的一个独特有效皂化反应器23C产生的使用无水氢氧化原位到获得2.最后,倒数第二个核心酸2与磺酰胺3的偶联提供了药物1始终如一的高质量.还将详细讨论关键的pd催化的c-n交叉耦合的挑战和解决方案.改进的合成技术克服了许多最初的扩大规模挑战,并以3,3-二甲基二环己酮(6)的46%的总收率实现,是第一代路线总收率的两倍多.成功实施了新工艺,以生产面积纯度大于99%的1.
Doi:10.1021/acs.Joc.8B02750

专利信息

专利号:US-2022073513-A1
优先权日:2018-12-29
标题:1h-pyrrolo[2,3-b]pyridine derivatives and related compounds as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases
发明人：CHEN YI
权利人:NEWAVE PHARMACEUTICAL INC
摘要:The present invention relates to compounds of Formula (II) and more preferably to 1H-pyrrolo[2,3-b]pyridine derivatives of formula (III) and related compounds. The variables are defined in the claims. The compounds are BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis of exemplary compounds as well as pharmacological data thereof (pages 61 to 72; examples 1 to 4; tables). An exemplary compound is e.g. 4-(4-[[2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-en-1-yl]methyl]piperazin-1-yl)-2-[methyl(1H-pyrrolo[2,3-b]pyridin-5-yl)phosphoroso]-N-[3-nitro-4-[(oxan-4-yl methyl)amino]benzenesulfonyl]benzamide (example 1).

专利号:US-2023119463-A1
优先权日:2019-12-27
标题 :1h-pyrrolo[2,3-b]pyridine derivatives as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases
发明人：CHEN YI
权利人:NEWAVE PHARMACEUTICAL INC
摘要:The present invention relates to 1H-pyrrolo[2,3-b]pyridine derivatives and related compounds as BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 162 to 233; examples 1 to 8; table; compound examples cpd-1 to cpd-135; biological examples 1 to 4).

专利号:WO-2021133817-A1
优先权日:2019-12-27
标题 :1h-pyrrolo[2,3-b]pyridine derivatives as bcl-2 inhibitors for the treatment of neoplastic and autoimmune diseases
发明人：CHEN YI
权利人:GUANGZHOU LUPENG PHARMACEUTICAL COMPANY LTD; NEWAVE PHARMACEUTICAL INC
摘要:The present invention relates to lH-pyrrolo[2,3-b]pyridine derivatives and related compounds as BCL-2 inhibitors for treating neoplastic, autoimmune or neurodegenerative diseases. The present description discloses the synthesis and characterisation of exemplary compounds as well as pharmacological data thereof (e.g. pages 162 to 233; examples 1 to 8; table; compound examples cpd-1 to cpd-135; biological examples 1 to 4).