CAS: 79538-29-7; 2,4,6-Trifluorobenzoylchloride

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CAS号28314-80-9 2,4,6-三氟苯甲酸 | CAS号1201597-19-4 4-(2,4,6-三氟苯甲酰基... | CAS号439239-90-4 2,4,6-三氟-N-[6-[...

2,4,6-三氟苯甲酸置于氯化亚砜体系中,用 甲苯 作为反应溶剂,化学反应 2.0H,反应生成 2,4,6-三氟苯甲酰氯
参考文献:几种卤代非硝基苯并噻嗪酮的合成,结构表征和抗分枝杆菌评价
标题:几种卤代非硝基苯并噻嗪酮的合成,结构表征和抗分枝杆菌评价
摘要:8-Nitro-1,3-Benzothiazin-4-Ones (Btzs),以 Btz043 和 Pbtz169 为最先进的化合物,代表了一类新的强效抗结核药物,可不可逆地抑制癸二烯基磷酰-β-D-核糖-2'-差向异构酶 (Dpre1),一种对病原体结核分枝杆菌细胞壁合成至关重要的酶.金分枝杆菌dsm 43999 和结核分枝杆菌h 37的合成,结构表征和体外测试报道了缺少硝基的卤代 2-(4-Ethoxycarbonylpiperrazin-1-yl)-1,3-Benzothiazin-4-Ones 的 Rv.x 射线晶体学显示 Btz 支架的结构可以显着偏离平面性.与最近的报道相反,本研究的结果表明,进一步研究卤代非硝基 Btz 的抗结核活性并不是一种有前途的方法.
DOI:10.1007/s00044-021-02735-4

专利信息

专利号:US-8697876-B2
优先权日:2010-04-02
标 题:Compositions and methods of synthesis of pyridinolypiperidine 5-HT1F agonists
发明人：CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN
权利人:CARNIAUX JEAN-FRANCOIS; CUMMINS JONATHAN; COLUCID PHARMACEUTICALS INC
摘要:The present invention provides a novel polymorph of the hemisuccinate salt of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide (Form A) characterized by a unique X-ray diffraction pattern and Differential Scanning Calorimetry profile, as well as a unique crystalline structure. This polymorph is useful in pharmaceutical compositions, for example, for the treatment and prevention of migraine. The invention also provides a process for the synthesis of pyridinoylpiperidine compounds of Formula I in high yield and high purity. In particular, the provides a process for the preparation of 2,4,6-trifluoro-N-[6-(1-methyl-piperidine-4-carbonyl)-pyridin-2-yl]-benzamide, its hemisuccinate salt and polymorph (Form A).

专利号:US-12172977-B2
优先权日:2019-07-01
标题:2,2-dimethyl-n-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propionamide, method for preparing (6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone using said compound, and use of said compound in the preparation of lasmiditan
发明人：ARE CELESTE; SÃ?NCHEZ CASALS CARLES; DOBARRO RODRÃ?GUEZ ALICIA
权利人:MOEHS IBERICA SL
摘要:The present invention relates to a new intermediate, (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide) useful in the synthesis of lasmiditan, to a method for obtaining same, to the use of said intermediate for preparing lasmiditan, to a method for preparing lasmiditan making use of said intermediate, and to a method for preparing an intermediate ((6-amino-pyridin-2-yl)-(1-methyl-piperidin-4-yl)-methanone) from (2,2-dimethyl-N-[6-(1-methyl-piperidin-4-carbonyl)-pyridin-2-yl]-propanamide).

专利号:US-8748459-B2
优先权日:2002-03-29
标 题 :Pyridinoylpiperidines as 5-HT1F agonists
发明人：COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI
权利人:COHEN MICHAEL PHILIP; KOHLMAN DANIEL TIMOTHY; LIANG SIDNEY XI; VICTOR FRANTZ; XU YAO-CHANG; YING BAI-PING; ZACHERL DEANNA PIATT; ZHANG DEYI; LILLY CO ELI
摘要:The present invention relates to compounds of formula I: n nor pharmaceutically acceptable acid addition salts thereof, where;n R 1 is C 1 -C 6 alkyl, substituted C 1 -C 6 alkyl, C 3 -C 7 cycloalkyl, substituted C 3 -C 7 cycloalkyl, C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, substituted C 3 -C 7 cycloalkyl-C 1 -C 3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R 2 is hydrogen, C 1 -C 3 alkyl, C 3 -C 6 cycloalkyl-C 1 -C 3 alkyl, or a group of formula II nn n n n n n n n n n n n R 3 is hydrogen or C 1 -C 3 alkyl; n R 4 is hydrogen, halo, or C 1 -C 3 alkyl; n R 5 is hydrogen or C 1 -C 3 alkyl; n R 6 is hydrogen or C 1 -C 6 alkyl; and n n is an integer from 1 to 6 inclusively. n n n n n The compounds of the present invention are useful for activating 5-HT lF receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.

专利号:US-2013072524-A1
优先权日:2010-04-02
标 题 :Compositions And Methods Of Synthesis Of Pyridinolypiperidine 5-HT1F Agonists

专利号:CA-2795062-A1
优先权日:2010-04-02
标 题 :Compositions and methods of synthesis of pyridinoylpiperidine 5-ht1f agonists

专利号:WO-2011123654-A1
优先权日:2010-04-02
标题 :Compositions and methods of synthesis of pyridinoylpiperidine 5-ht1f agonists