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CAS号504-30-3 3-羟基哒嗪 | CAS号10025-87-3 三氯氧磷 | CAS号5469-70-5 3-氨基哒嗪 | CAS号40972-16-5 3-肼基哒嗪盐酸盐 | CAS号289-80-5 哒嗪 | CAS号135034-10-5 3-氯-6-碘哒嗪 | CAS号19064-65-4 3-甲氧基嘧啶 | CAS号65202-53-1 3-Iodopyridazine | CAS号871020-44-9 (9ci)-3-甲基-4-(3... | CAS号62567-44-6 3-乙氧基哒嗪合成工艺路线路线简述
- 合成目标产物 3-Chloropyridazine 主要起始原料 3(2H)-Pyridazinone
- (文献来源)合成步骤主要原料 3(2H)-Pyridazinone
3-哒嗪酮置于三氯氧磷体系中,化学反应 1.5H,以73%的收率获得3-氯哒嗪
参考文献:卤代杂芳烃向钯(0)的氧化加成:协同作用与snar型机理
标题:卤代杂芳烃向钯(0)的氧化加成:协同作用与snar型机理
摘要:在thf和dmf中研究了卤代杂芳芳烃hetx(x = I,Br,Cl)氧化成[pd 0(pph 3)2 ](由[pd 0(pph 3)4 ]产生)的动力学.速率常数已确定.与此相反的普遍接受的协调机制,为取代的2-卤代吡啶和溶剂效应得到哈米特曲线揭示了依赖于hetx的卤化物x的反应机理:一个前所未有的小号ñ对于x = Br或cl和经典协调一致的ar型机构x = I的机制.这些结果得到dft研究的支持.
Doi:10.1002/chem.201406210
专利信息
专利号:US-7220858-B2
优先权日:2003-12-23
标 题 :Synthesis of hydrazine and chlorinated derivatives of bicyclic pyridazines
发明人:NELSON DEANNA J
权利人:BARBEAU PHARMA INC
摘要:The present invention relates to both a novel method of preparing hydralazine hydrochloride and to a novel method of preparing hydrazine derivatives of compounds containing a pyridazine ring, including, for example, pyridazines, phthalazines and other compounds containing the pyridazine ring.
专利号:WO-0107416-A1
优先权日:1999-07-28
标题 :Method of producing pyridazine carboxylic acid derivatives
发明人:BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
权利人:LONZA AG; BESSARD YVES; CRETTAZ ROGER; EGGEL MICHAEL
摘要:The invention relates to a method of producing pyridazine carboxylic acid derivatives of the general formulae (Ia) or (Ib), wherein R<1> represents a group of the formula -OR<3> or -NR<4>R<5>, R<2> represents hydrogen, chlorine, a group of the formula -OR<6> or a group of the formula -NR<7>R<8>, R<3> represents C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl, R<4> represents C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl, R<5> represents hydrogen, C1-10 alkyl, C3-8 cycloalkyl, optionally substituted aryl or aryl-C1-4-alkyl and R<6> represents C1-10 alkyl, C3-8 cycloalkyl, aryl-C1-4-alkyl or an optionally substituted aromatic or heteroaromatic rest and R<7> and R<8> represent independently C1-10 alkyl, C3-8 cycloalkyl or aryl-C1-4-alkyl or together with the nitrogen atom form a saturated or aromatic heterocyclic ring. The inventive derivatives are obtained by reacting the corresponding 3-chloropyridazines or 3,6-dichloropyridazine with carbon monoxide and alcohols or amines H-R<1> in the presence of palladium-phosphin complexes and bases. The pyridazine carboxylic acid derivatives (Ia, Ib) are the intermediates for the synthesis of pharmaceutically active substances.
专利号:US-2005137397-A1
优先权日:2003-12-23
标题:Synthesis of hydrazine derivatives of pyridazine
专利号:US-2010004245-A1
优先权日:2006-10-20
标 题:Azacycloalkane derivatives as inhibitors of stearoyl-coenzyme a delta-9 desaturase
发明人:OBALLA RENATA M; DESCHENES DENIS; GAGNON MARC; LEBLANC YVES; POWELL DAVID; RAMTOHUL YEEMAN K
权利人:MERCK FROSST CANADA LTD
摘要:Azacycloalkane derivatives of structural formula (I) are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.
专利号:WO-2023091726-A1
优先权日:2021-11-18
标题:Inhibitors of cyclin‑dependent kinase 12 (cdk12)
发明人:BENOIT GUILLAUME; CARULLI JOHN; CHEN FEI; CHUAQUI CLAUDIO; CIBLAT STEPHANE; COOPER ELLIOT; DAGENAIS ROBIN; HU SHANHU; KABRO ANZHELIKA; LAPLACA DEREK; MARINEAU JASON; MOEBIUS DAVID; MOON DIANE; SOLODININ ANDREI; WHITMORE KENNETH
权利人:SYROS PHARMACEUTICALS INC
摘要:The present invention provides chemical compounds that inhibit one or more families of kinases (e.g., serine/threonine kinases, including one or more of the families of CDK proteins, and in particular, CDK12). More specifically, the present invention provides CDK12 inhibitors, of formula (I), pharmaceutically acceptable salts and isotopically labeled derivatives thereof, pharmaceutical compositions containing the compounds/inhibitors, and methods of their synthesis and use in treating proliferative diseases (e.g., a bladder cancer, a breast cancer, Ewing's sarcoma, a gastric cancer, a gastrointestinal cancer, a hematologic cancer, a lung cancer (e.g., small cell lung cancer (SCLC)), an ovarian cancer (e.g., a high grade serous ovarian cancer), a pancreatic cancer (e.g., pancreatic ductal adenocarcinoma (PDAC)), a brain cancer (e.g., glioblastoma), or a prostate cancer), alone or in combination with a second therapeutic agent. The proliferative disease can be a cancer, benign neoplasm, or pathologic angiogenesis, and any of the therapeutic methods or uses described herein can include a step of diagnosing the patient's disease. In other embodiments of the invention, the compositions described herein (e.g., the compounds, pharmaceutical compositions, and kits containing them) are used for the treatment of myotonic dystrophy (type 1 or type 2).
专利号:US-2008119524-A1
优先权日:2002-08-14
标题 :Prenylation inhibitors containing dimethylcyclobutane and methods of their synthesis and use
发明人:BROWN BRADLEY B; REHDER KENNETH S; STRACHAN JON-PAUL; EAVES JERON H; LOWDEN CHRISTOPHER T
权利人:BROWN BRADLEY B; REHDER KENNETH S; STRACHAN JON-PAUL; EAVES JERON H; LOWDEN CHRISTOPHER T
摘要:The present invention is directed to compounds useful in the treatment of diseases associated with prenylation of proteins and pharmaceutically acceptable salts thereof, to pharmaceutical compositions comprising same, and to methods for inhibiting protein prenylation in an organism using the same.