CAS: 16234-10-9; Thieno[3,2-D]Pyrimidin-4(3H)-One

相似化合物

18678-13-2 1245811-20-4 16233-51-5

上下游产品

CAS号22288-78-4 3-氨基-2-噻吩甲酸甲酯 | CAS号149-73-5 原甲酸三甲酯 | CAS号64-18-6 甲酸 | CAS号77287-34-4 甲亚胺酸 | CAS号109-86-4 乙二醇甲醚 | CAS号147123-47-5 3-氨基噻吩-2-羧酰胺 | CAS号31823-64-0 3-氨其噻吩-2-甲酸乙酯 | CAS号272-68-4 噻吩并[3,2-D]嘧啶 | CAS号31169-25-2 7-溴噻吩并[3,2-d]嘧啶... | CAS号31169-27-4 7-溴-4-氯噻酚并[3,2-D]嘧啶 | CAS号225385-03-5 6-溴-4-氯噻吩[3,2-D]嘧啶 | CAS号1318133-32-2 7-溴噻吩并[3,2-D]嘧啶-4-胺 | CAS号16290-53-2 (4-oxothieno[3,... | CAS号16229-26-8 4-Hydrazinothie... | CAS号1269667-57-3 4-氯噻吩并[3,2-d]嘧啶-7-羧酸 | CAS号16269-66-2 4-氯噻吩并[3,2-d]嘧啶 | CAS号21586-25-4 7-溴噻吩并[3,2-d]嘧啶

Methyl 3-Formamidothiophene-2-Carboxylate置于甲酸铵,Formamide体系中,化学反应 4.0H,以86%的收率获得1,4-二氢噻吩并[3,2-D]嘧啶-4-酮
参考文献:表皮生长因子受体的不可逆抑制剂:具有 α,β-不饱和酰胺侧链的噻吩并嘧啶核
标题:表皮生长因子受体的不可逆抑制剂:具有 α,β-不饱和酰胺侧链的噻吩并嘧啶核
摘要:表皮生长因子受体 (Egfr) 酪氨酸激酶的过度表达已在多种癌症中发现,例如乳腺癌,卵巢癌,结肠癌和非小细胞肺癌,这与患者的不良预后有关.为了寻找有效的 Egfr 酪氨酸激酶家族(主要是 Her2)的不可逆抑制剂,以噻吩并 [3,2-D] 吡啶和噻吩并 [2,3-D] 吡啶为中心部分的两个系列 Her2 酪氨酸激酶抑制剂和开发了具有碱性α,β-不饱和酰胺侧链的化合物.位于 6 位的 α,β-不饱和酰胺侧链(迈克尔受体)与位于 Egfr 酶的 Atp 结合口袋中的 Cys773 形成共价键,是产生不可逆抑制的主要因素.在我们的研究中,使用噻吩并嘧啶代替喹唑啉作为中心结构,并在4位引入不同的取代基以研究构效关系.噻吩并[2,3-D]嘧啶衍生物16A-D对sk-Br-3细胞显示出有效的her2酶抑制和抗增殖活性.特别是,(E)-N-(4-((3-Chloro-4-(Pyridin-2-Ylmet
Doi:10.1002/ardp.201400098

专利信息

专利号:US-11524957-B2
优先权日:2018-04-02
标 题 :Process for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4(3H)-one
发明人：ZHU LEI; BAILEY JOHN DANIEL; DURAK LANDON; WAETZIG JOSHUA DAVID; MIZUNO MASAHIRO; MAEDA KAZUHIRO; YASUMA TSUNEO; YAMAGUCHI HIROSHI; FUKUOKA KOICHIRO; AKIYAMA KAZUYUKI
权利人:TAKEDA PHARMACEUTICALS CO
摘要:The present invention provides processes and synthetic intermediates for the synthesis of 2-[(2S)-1-azabicyclo[2.2.2]oct-2-yl]-6-(3-methyl-1H-pyrazol-4-yl)thieno[3,2-d]pyrimidin-4 {3H)-one or a salt, hydrate, or tautomer thereof, or any combination thereof, which are Cdc7 kinase inhibitors, and are useful for the treatment of disorders of cell proliferation, particularly cancer, and other disorders associated with Cdc7 activity.

专利号:US-11999749-B2
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto
发明人：GOSSELIN FRANCIS; KOENIG STEFAN G; MERCADO-MARIN EDUARDO V; STUMPF ANDREAS; ZELL DANIEL; ZHANG HAIMING; BACHMANN STEPHAN; CARRERA DIANE E; DALZIEL MICHAEL E; GE YONGHUI; ZHANG JIE; BIGLER RAPHAEL; FINET LAURE ELIZABETH SIMONE; MONDIERE REGIS JEAN GEORGES; NAKAGAWA YUKI
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.

专利号:US-9085605-B2
优先权日:2010-05-27
标 题:Chemical synthesis and anti-tumor and anti-metastatic effects of dual functional conjugate
发明人：LIU GANG; ZHAO NAN; MA YAO
权利人:LIU GANG; ZHAO NAN; MA YAO; SHENZHEN SALUBRIS PHARM CO LTD
摘要:The present invention discloses chemical synthesis, anti-tumor and anti-metastatic effects of a dual functional conjugate as shown by formula I. Specifically, paclitaxel or docetaxol is linked with muramyl dipeptide derivative to form a conjugate, thus dual anti-tumor and anti-metastatic effects are achieved by combination of chemotherapy and immunotherapy. The present invention also discloses that paclitaxel or docetaxol and muramyl dipeptide derivative conjugate is synthesized by combination of solid-phase and solution-phase synthesis, and said conjugate can be used in manufacture of anti-tumor medicaments as proved by reliable bioassays.

专利号:US-2025051351-A1
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto

专利号:US-2023028651-A1
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto

专利号:TW-202311265-A
优先权日:2021-06-30
标 题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto