3-溴-5-甲氧基吡啶置于1,1'-双(二苯膦基)二茂铁二氯化钯(II)二氯甲烷复合物,硫酸,水,Potassium Acetate,三乙酰氧基硼氢化钠,Potassium Carbonate,Caesium Carbonate,三乙胺,N,N-二异丙基乙胺,Sodium Hydroxide,十二硫醇体系中,用 四氢呋喃,1,4-二氧六环,二氯甲烷,水,二甲基亚砜,N,N-二甲基甲酰胺,异丙醇,乙腈 用作溶剂,化学反应 129.0H,反应生成塞卡替尼 参考文献:Process For The Preparation Of 6-(2-Hydroxy-2-Methylpropoxy)-4-(6-(6-((6-Methoxypyridin-3-yl)Methyl)-3,6-Diazabicyclo[3.1.1]Heptan-3-yl)Pyridin-3-yl)Pyrazolo[1,5-A]Pyridine-3-Carbonitrile 标题:Process For The Preparation Of 6-(2-Hydroxy-2-Methylpropoxy)-4-(6-(6-((6-Methoxypyridin-3-yl)Methyl)-3,6-Diazabicyclo[3.1.1]Heptan-3-yl)Pyridin-3-yl)Pyrazolo[1,5-A]Pyridine-3-Carbonitrile 摘要:在某些实施例中,本文提供了一种制备如本文所述的公式i化合物或其药用可接受盐的过程.
专利号:US-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-3959322-A 优先权日:1960-09-22 标 题:Synthesis of 13-alkyl-gon-4-ones 发明人:HUGHES GORDON ALAN; SMITH HERCHEL 权利人:SMITH HERCHEL 摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:US-5656634-A 优先权日:1991-03-21 标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 发明人:CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:WO-2011032359-A1 优先权日:2009-09-17 标题:Momordica charantia peptide mc-jj6 and microwave promoted solid phase synthesis method thereof 发明人:HUANG WENLONG; JIN JING; QIAN HAI; ZHANG HUIBIN; CHEN WEI; WANG JINGJIE; DU KUO 权利人:UNIV CHINA PHARMA; HUANG WENLONG; JIN JING; QIAN HAI; ZHANG HUIBIN; CHEN WEI; WANG JINGJIE; DU KUO 摘要:Provided are peptides MC-JJ6 and MC-JJ6222 from Momordica charantia with hypoglycemic activity and a microwave promoted solid phase synthesis method thereof. The peptides MC-JJ6 and MC-JJ6222 comprise the amino acid sequences of SEQ ID NO: 1 and SEQ ID NO: 115, respectively.
专利号:WO-2011032360-A1 优先权日:2009-09-17 标 题:Momordica charantia peptide mc-jj2 and microwave promoted solid phase synthesis method thereof 发明人:HUANG WENLONG; JIN JING; QIAN HAI; ZHANG HUIBIN; CHEN WEI; WANG JINGJIE; DU KUO 权利人:UNIV CHINA PHARMA; HUANG WENLONG; JIN JING; QIAN HAI; ZHANG HUIBIN; CHEN WEI; WANG JINGJIE; DU KUO 摘要:Provided are peptides MC-JJ2 and MC-JJ2163 from Momordica charantia with hypoglycemic activity and a microwave promoted solid phase synthesis method thereof. The peptides MC-JJ2 and MC-JJ2163 comprise the amino acid sequences of SEQ ID NO: 1 and SEQ ID NO: 108, respectively.
1: Russo A, Lopes AR, McCusker MG, Garrigues SG, Ricciardi GR, Arensmeyer KE, Scilla KA, Mehra R, Rolfo C. New Targets in Lung Cancer (Excluding EGFR, ALK, ROS1). Curr Oncol Rep. 2020 Apr 16;22(5):48. doi: 10.1007/s11912-020-00909-8. 15(4):541-549. doi: 10.1016/j.jtho.2020.01.006. Epub 2020 Jan 24. 16(2):77-78. doi: 10.1038/s41574-019-0307-2. 25(12):1839-1842. doi: 10.1038/s41591-019-0653-6. Epub 2019 Nov 25. 7: Li AY, McCusker MG, Russo A, Scilla KA, Gittens A, Arensmeyer K, Mehra R, Adamo V, Rolfo C. RET fusions in solid tumors. Cancer Treat Rev. 2019 Dec;81:101911. doi: 10.1016/j.ctrv.2019.101911. Epub 2019 Oct 30. 29(11):1704-1707. doi: 10.1089/thy.2019.0041. 12:7857-7864. doi: 10.2147/OTT.S171665.
合成参考文献
参考文献:10.1016/j.oraloncology.2020.104973 摘要:Wei D, Chen D, Li L, Tian J, Ren G. ALG8-RET: A novel RET rearrangement in a patient with malignant melanoma of the palatal mucosal. Oral Oncol. 2020 Dec;111():104973. doi: 10.1016/j.oraloncology.2020.104973. 参考文献:10.1038/s41698-021-00214-y 摘要:Mansfield AS, Hong DS, Hann CL, Farago AF, Beltran H, Waqar SN, Hendifar AE, Anthony LB, Taylor MH, Bryce AH, Tagawa ST, Lewis K, Niu J, Chung CH, Cleary JM, Rossi M, Ludwig C, Valenzuela R, Luo Y, Aggarwal R. A phase I/II study of rovalpituzumab tesirine in delta-like 3—expressing advanced solid tumors. npj Precision Oncology. 2021 Aug 05;5(1):74. doi: 10.1038/s41698-021-00214-y. 参考文献:10.1007/s10549-021-06452-9 摘要:Pavanelli AC, Mangone FR, Yoganathan P, Bessa SA, Nonogaki S, de Toledo Osório CAB, de Andrade VP, Soares IC, de Mello ES, Mulligan LM, Nagai MA. Comprehensive immunohistochemical analysis of RET, BCAR1, and BCAR3 expression in patients with Luminal A and B breast cancer subtypes. Breast Cancer Research and Treatment. 2022 Jan 15;192(1):43–52. doi: 10.1007/s10549-021-06452-9. 参考文献:10.1200/po.20.00282 摘要:Watanabe S, Takeda M, Otani T, Yoshida T, Sakai K, Olek E, Rothenberg SM, Kherani J, French PP, Nishio K, Ito A, Nakagawa K. Complete Response to Selective RET Inhibition With Selpercatinib (LOXO-292) in a Patient With RET Fusion–Positive Breast Cancer. JCO Precision Oncology. 2021 Nov;(5):103–6. doi: 10.1200/po.20.00282. 参考文献:10.1200/po.21.00127 摘要:Mweempwa A, Xu H, Vissers JHA, Tothill RW, Pattison AD, Fellowes AP, Thomas DM, Richardson G, Hicks RJ, Grimmond SM, Fox SB, Luen SJ, Desai J, Solomon BJ. Novel RET Fusion RET-SEPTIN9 Predicts Response to Selective RET Inhibition With Selpercatinib in Malignant Pheochromocytoma. JCO Precis Oncol. 2021 Nov;5():1160–5. doi: 10.1200/po.21.00127.