CAS: 36082-50-5; 5-Bromo-2,4-Dichloropyrimidine

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63931-21-5 56181-39-6 68797-61-5

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CAS号51-20-7 5-溴脲嘧啶 | CAS号113138-12-8 5-bromo-2-thiox... | CAS号10026-13-8 五氯化磷 | CAS号10025-87-3 三氯氧磷 | CAS号56686-16-9 5-溴-2,4-二甲氧基嘧啶 | CAS号57054-92-9 2-氯-4-甲氧基-5-溴嘧啶 | CAS号59549-51-8 5-溴-2-氯-4-(甲硫基)嘧啶 | CAS号57054-86-1 5-溴-2-氯-N,N-二甲基... | CAS号41244-53-5 2,4-双(苄氧基)-5-溴嘧啶 | CAS号51-20-7 5-溴脲嘧啶 | CAS号66-22-8 尿嘧啶 | CAS号51-21-8 5-氟尿嘧啶 | CAS号205672-24-8 5-溴-2-氯-N-甲基嘧啶-4-胺 | CAS号205672-19-1 5-溴-2-氯-4-(苯基甲氧基)-嘧啶

5-溴尿嘧啶置于三氯氧磷体系中,化学反应 4.0H,反应生成 5-溴-2,4-二氯嘧啶
参考文献:2,4-Dialkoxy-5-Bromopyrimidine 的金属化和二甲基甲酰胺的甲酰化:2,6-Dialkoxy-5-Dimethylaminopyrimidine-4-Carboxaldehyde 的分离
标题:2,4-Dialkoxy-5-Bromopyrimidine 的金属化和二甲基甲酰胺的甲酰化:2,6-Dialkoxy-5-Dimethylaminopyrimidine-4-Carboxaldehyde 的分离
摘要:2,4-二烷氧基-5-溴嘧啶与二异丙基氨基锂直接金属化,随后被二甲基甲酰胺捕获,通过二甲基甲酰胺的二甲胺部分置换溴,出人意料地形成了 2,6-二烷氧基-5-二甲氨基嘧啶-4-甲醛.
DOI:10.1080/00397910903175397

专利信息

专利号:US-10981922-B2
优先权日:2012-04-26
标题 :Synthesis of lactams
发明人：TAVARES FRANCIS XAVIER
权利人:TAVARES FRANCIS XAVIER
摘要:Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC—OR—NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam.

专利号:US-2016257688-A1
优先权日:2013-10-24
标 题 :Process for Synthesis of Lactams
发明人：TAVARES FRANCIS XAVIER
权利人:TAVARES FRANCIS XAVIER
摘要:Methods for the synthesis of lactams are presented whereby a carboxylic acid of the formula HOOC—OR—NH-LG, wherein OR is an organic moiety and LG is a leaving group, is reacted with an acid, such as an organic acid, in particular a strong acid, and a dehydrating agent, which may be one in the same such as a strong acid anhydride, such that the amount of acid added allows for the desired transformation to take place without the loss of the leaving group (LG) before the cyclization, and recovering the lactam such as that of the formula (a), provided herein, wherein G represents the atom(s) needed to form a closed ring.

专利号:US-5304647-A
优先权日:1988-02-09
标题:Method of preparation of halogenated diazines
发明人：STREKOWSKI LUCJAN; MOKROSZ MARIA; HARDEN DONALD B
权利人:UNIV GEORGIA STATE
摘要:A method of preparation of substituted halogenodiazines which are useful as intermediates in the synthesis of novel unfused heterobicyclic compounds, and the products thereof. The reaction consists of the addition of an organolithium reagent with subsequent dehydrogenation of the addition product. The reaction takes place in one reaction vessel, without isolation of the substituted halogenodihydrodiazine intermediate. The reactions proceed at moderate temperature and in a short amount of time, which decreases the probability of side reactions and increases yield. Furthermore, the workup step is conducted under two-phase conditions to prevent hydrolysis of the substituted halogenodiazine to a substituted hydroxydiazine. The method is easy, efficient and results in a high yield of product. The substituted halogenodiazines are used as intermediates in the synthesis of unfused heterobicyclic compounds containing an aromatic moiety, diazine, and another aromatic moiety, such as thiophene, benzene, or naphthalene, which have biological activity.

专利号:US-11629150-B2
优先权日:2016-07-01
标题:Synthesis of N-(heteroaryl)-pyrrolo[3,2-d]pyrimidin-2-amines
发明人：SMITH ALEXANDER; WHITE HANNAH S; TAVARES FRANCIS XAVIER; KRASUTSKY SERGIY; CHEN JIAN-XIE; DORROW ROBERTA L; ZHONG HUA
权利人:G1 THERAPEUTICS INC
摘要:This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers.

专利号:US-7897762-B2
优先权日:2006-09-14
标 题:Kinase inhibitors useful for the treatment of proliferative diseases
发明人：FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C
权利人:DECIPHERA PHARMACEUTICALS LLC
摘要:The present invention relates to novel kinase inhibitors and modulator compounds 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-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.