CAS: 723286-98-4; 5-(Chloromethyl)-2-(Trifluoromethyl)-1,3,4-Oxadiazole

相似化合物

1868-48-0 1036648-53-9 1260901-93-6

上下游产品

CAS号762240-99-3 1-氯乙酰基-2-(三氟乙酰基)肼 | CAS号1538-08-5 三氟乙酰肼 | CAS号79-04-9 氯乙酰氯 | CAS号723286-97-3 5,6,7,8-四氢-5,5-...

1-(氯乙酰基)-2-(三氟乙酰基)肼置于三氯氧磷体系中,用 乙腈 作为反应溶剂,以61 %的收率获得产物5-氯甲基-2-三氟甲基-1,3,4-噁二唑
参考文献:新型三唑并[4,3-A]吡嗪衍生物的合成及抗菌活性
标题:新型三唑并[4,3-A]吡嗪衍生物的合成及抗菌活性
摘要:传染病对人类健康构成重大挑战,迫切需要开发具有优异抗菌活性的新型抗菌药物.合成了一系列新型三唑并[4,3-A]吡嗪衍生物,并利用熔点,1H和13C核磁共振波谱,质谱和元素分析等技术对其结构进行了表征.使用微肉汤稀释法评价所有合成的化合物的体外抗菌活性.在所有测试的化合物中,一些化合物对革兰氏阳性金黄色葡萄球菌和革兰氏阴性大肠杆菌菌株均表现出中等至非常好的抗菌活性.特别是,化合物2E表现出优异的抗菌活性(mic:对金黄色葡萄球菌的mic为32 μg/ml,对大肠杆菌的mic为16 μg/ml),与一线抗菌剂氨苄青霉素相当.此外,还初步研究了三唑并[4,3-A]吡嗪衍生物的构效关系.
DOI:10.3390/molecules28237876

专利信息

专利号:US-7468459-B2
优先权日:2003-03-19
标题:Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
发明人：XIAO YI; ARMSTRONG III JOSEPH D; KRSKA SHANE W; NJOLITO EUGENIA; RIVERA NELO R; SUN YONGKUI; ROSNER THORSTEN
权利人:MERCK & CO INC
摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

专利号:US-7495123-B2
优先权日:2004-04-05
标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives
发明人：XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE
权利人:SOLVIAS AG; MERCK & CO INC
摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

专利号:WO-2004083212-A1
优先权日:2003-03-18
标 题:Process to beta-ketoamide intermediates to dipeptidyl peptidase inhibitors
发明人：IKEMOTO NORIHIRO; SIMMONS BRYON L; WILLIAMS J MICHAEL; XU FENG; YANG CHUNHUA
权利人:MERCK & CO INC; IKEMOTO NORIHIRO; SIMMONS BRYON L; WILLIAMS J MICHAEL; XU FENG; YANG CHUNHUA
摘要:A novel process is provided for the preparation of beta-ketoamide intermediates which are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of type 2 diabetes. Also provided are useful intermediates obtained from the process.

专利号:CN-113527312-A
优先权日:2021-08-24
标题 :A kind of green synthesis method of sitagliptin intermediate

专利号:CN-113527312-B
优先权日:2021-08-24
标 题:Green synthesis method of sitagliptin intermediate