CAS: 42831-50-5; 5-Methylisoxazole-4-Carboxylic Acid

相似化合物

42831-50-5 51135-73-0 2510-36-3

上下游产品

CAS号51135-73-0 5-甲基-4-异噁唑甲酸乙酯 | CAS号134653-70-6 2-Dimethylamino... | CAS号3788-94-1 2-乙氧亚甲基乙酰乙酸乙酯 | CAS号100367-49-5 (5-甲基异恶唑-4-基)甲醇 | CAS号33142-24-4 2-甲酰基-3-氧代丁酸乙酯 | CAS号75706-12-6 来氟米特 | CAS号67305-24-2 5-甲基-4-异恶唑羰基氯 | CAS号99803-72-2 那巴卡朵

5-甲基-4-异噁唑甲酸乙酯置于硫酸体系中,用 水 作为反应溶剂,化学反应 20.0H,以60%的收率获得产物5-甲基异恶唑-4-甲酸
参考文献:新型来氟米特类似物的合成及体内抗纤维化活性
标题:新型来氟米特类似物的合成及体内抗纤维化活性
摘要:合成了新型来氟米特类似物,并在体内针对硫代乙酰胺(taa)诱导的大鼠肝纤维化进行了评估.与使用来氟米特治疗的动物相比,用新类似物治疗的所有动物均显示出提高的或相当的存活率.用化合物8D,8E,9和11治疗的动物显示出比来氟米特治疗的动物改善的肝脏参数.肝脏的组织病理学研究表明,化合物8A是活性最高的化合物,可将纤维化降低至最低水平,化合物8C,8E和11是纤维化评分为2-3的活性化合物,优于来氟米特.
DOI:10.2174/1570180813666160630125624

专利信息

专利号:US-10526279-B2
优先权日:2015-06-17
标题:Process for the preparation of teriflunomide
发明人：Palle Venkata Raghavendracharyulu; BHAT RAMAKRISHNA PARAMESHWAR; KALIAPPAN MARIAPPAN; BABU JITHENDRA R; SHANMUGHASAMY RAJMAHENDRA
权利人:BIOCON LTD
摘要:The present invention provides a process for the preparation of Teriflunomide (Formula-I). The present invention describes the synthesis of Teriflunomide without isolating the intermediate Leflunomide. Teriflunomide is prepared from 5-Methyl isoxazole-4-carboxylic acid by converting to its acid chloride and coupling with 4-trifluoromethyl aniline to obtain Leflunomide (which is not isolated) followed by ring opening reaction using aq. Sodium Hydroxide to form Teriflunomide. In other words, the process is telescoped from 5-methylisoxazole-4-carbonyl chloride.

专利号:US-2007275962-A1
优先权日:2003-09-10
标 题:Heterobicyclic Compounds as Pharmaceutically Active Agents
发明人：KOUL ANIL; KLEBL BERT; MULLER GERHARD; MISSIO ANDREA; SCHWAB WILFRIED; HAFENBRADL DORIS; NEUMANN LARS; SOMMER MARC-NICOLA; MULLER STEFAN; HOPPE EDMUND; FREISLEBEN ACHIM; BACKES ALEXANDER; HARTUNG CHRISTIAN; FELBER BEATRICE; ZECH BIRGIT; ENGKVIST OLA; KERI GYORGY; ORFI LASZLO; BANHEGYI PETER; GREFF ZOLTAN; HORVATH ZOLTAN; VARGA ZOLTAN; MARKO PETER; PATO JANOS; SZABADKAI ISTVAN; SZEKELYHID ZSOLT; WACZEK FRIGYES
权利人:GPC BIOTECH AG
摘要:Described are heterobicyclic compounds such as 4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]thiopyran 3-carboxylic acid amides, 4,7-dihydro-5H-thieno[2,3-c]pyran-3-carboxylic acid amides, or benzo[b]thiophene-3-carboxylic acid amides and pharmaceutically acceptable salts thereof, the use of these derivatives for the prophylaxis and/or treatment of various diseases such as infectious diseases, including mycobacteriainduced infections and opportunistic diseases, prion diseases, immunological diseases, autoimmune diseases, bipolar and clinical disorders, cardiovascular diseases, cell proliferative diseases, diabetes, inflammation, transplant rejections, erectile dysfunction, neurodegenerative diseases and stroke, as well as compositions containing at least one heterobicyclic compound and/or pharmaceutically acceptable salts thereof. Furthermore, reaction procedures for the synthesis of the heterobicyclic compound are disclosed.

专利号:HU-P0301865-A2
优先权日:2000-02-15
标 题 :A process for the synthesis of leflunomide

专利号:US-9782406-B2
优先权日:2011-10-25
标 题 :Kinase inhibitor and method for treatment of related diseases
发明人：PAN ZHENGYING; LI XITAO
权利人:UNIV PEKING SHENZHEN GRADUATE SCHOOL; BEIJING RECIPROCAPHARMACEUTICALS CO LTD; BEIJING RECIPROCAPHARMACEUTICALS CO LTD
摘要:Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.

专利号:US-9150522-B2
优先权日:2011-10-25
标 题:Kinase inhibitor and method for treatment of related diseases
发明人：PAN ZHENGYING; LI XITAO
权利人:UNIV PEKING SHENZHEN GRAD SCHO; BEIJING RECIPROCAPHARMACEUTICALS CO LTD
摘要:Disclosed is a compound of (aminophenylamino) pyrimidyl benzamides and a synthesis method thereof. The compound has Btk-inhibition activity and can be used to treat autoimmune diseases, heteroimmune diseases, cancers or thromboembolic diseases.

专利号:ES-2237553-T3
优先权日:2000-02-15
标题 :PROCEDURE FOR THE SYNTHESIS OF LEFLUNOMIDE.