CAS: 849937-96-8; 5-Bromo-2,4-Dichloropyridine

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上下游产品

CAS号53939-30-3 5-溴-2-氯吡啶 | CAS号80791-79-3 3-溴-2,4-二羟基吡啶 | CAS号857730-21-3 4-氨基-5-溴-2-氯吡啶 | CAS号735255-56-8 4-氯-N,N-二甲基吡啶-2-胺

5-溴-2-氯吡啶置于正丁基锂,二异丙胺,1,1,2-三氯三氟乙烷(cfc-113)体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 1.5H,以83%的收率获得产物2,4-二氯-5-溴吡啶
参考文献:Regiochemically Flexible Substitutions Of Di-,Tri-,And Tetrahalopyridines: The Trialkylsilyl Trick
标题:Regiochemically Flexible Substitutions Of Di-,Tri-,And Tetrahalopyridines: The Trialkylsilyl Trick
摘要:2,4-Difluoropyridine,2,4-Dichloropyridine,2,4,6-Trifluoropyridine,2,4,6-Trichloropyridine And 2,3,4,6-Tetrafluoropyridine React With Standard Nucleophiles Exclusively At The 4-Position Under Halogen Displacement. However,The Regioselectivity Can Be Completely Reversed If A Trialkylsilyl Group Is Introduced In The 5-Position Of The 2,4-Dihalopyridines Or In The 3-Position Of The 2,4,6-Trihalopyridines Or 2,3,4,6-Tetrahalopyridine. Then Only The Halogen Most Remote From The Bulky Silyl Unit (At The 2-Position In The Case Of The 2,4-Halopyridines,At The 6-Position With The Other Substrates) Gets Involved In The Exchange Process. After Removal Of The Silyl Protective Group The Nucleophile Is Invariably Found To occupy The Nitrogen-Neighboring Position.
DOI:10.1021/jo047962Z

专利信息

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.