CAS: 103949-58-2; 3,4-Dichloro-2-Methylpyridine

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CAS号97944-40-6 3-氯-2-甲基吡啶-4-胺 | CAS号18437-58-6 4-氨基-2-甲基吡啶 | CAS号108004-98-4 2-Methyl-3,4-di... | CAS号103949-59-3 3,4-二氯-2-吡啶甲醇

📜2-甲基-4-氨基吡啶置于盐酸,硫酸,氯,Sodium Nitrite体系中,化学反应 5.0H,反应生成3,4-二氯-2-甲基吡啶
参考文献:2-[[((4-氨基-2-吡啶基)甲基]亚磺酰基]苯并咪唑h + / K +-Atpase抑制剂.吡啶碱度,稳定性和活性之间的关系.
标题:2-[[((4-氨基-2-吡啶基)甲基]亚磺酰基]苯并咪唑h + / K +-Atpase抑制剂.吡啶碱度,稳定性和活性之间的关系.
摘要:苯并咪唑亚砜类的分泌型h + / K +-Atpase抑制剂需要在中性生理条件下具有较高的稳定性,但在低ph下迅速重排至活性亚磺酰胺2.由于初始反应涉及吡啶氮的内部亲核攻击,因此吡啶的控制pka至关重要.在本文中,我们表明通过利用4-氨基取代基对吡啶的强大的供电子作用,并通过3-或5-卤素取代基的吸电子作用来缓和,这是一种高效能的组合(作为抑制剂在生理条件下可以获得组胺刺激的胃酸分泌)和非常好的稳定性.此外,举例说明了3/5取代基和4-取代基之间的空间相互作用在改变4-氨基的供电子能力中的作用,并确定了影响稳定性的其他因素.选择一种化合物,特别是2-[[[(3-氯-4-吗啉代-2-吡啶基)甲基]亚磺酰基]-5-甲氧基-(1H)-苯并咪唑(3A,Sk&f 95601)进行进一步开发和男人的评价.
Doi:10.1021/jm00128A046

专利信息

专利号:US-3933830-A
优先权日:1974-09-10
标 题 :Process for the synthesis of 4-(2-pyridylamido ethyl) piperidines
发明人：BARTH WAYNE E; KUHLA DONALD E
权利人:PFIZER
摘要:Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structure ##EQU1## wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms. n Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structure ##EQU2## with substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art. n The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.

专利号:US-3992388-A
优先权日:1974-09-10
标题 :4-(2-Pyridylamidoethyl)piperidines
发明人：BARTH WAYNE E; KUHLA DONALD E
权利人:PFIZER
摘要:Disclosed herein is an improved process for the preparation of known hypoglycemic piperidinesulfamylureas of the structue ##SPC1## n Wherein R is selected from the group consisting of 3-(2-methoxy)pyridyl, 3-(2-ethoxy)pyridyl and 2-(4-chloro)pyridyl and R' is selected from the group consisting of bicyclo[2.2.1]hept-5-en-2-yl-endo-methyl, bicyclo[2.2.1]hept-2-yl-endo-methyl, 7-oxabicyclo[2.2.1]hept-2-yl-methyl, 1-adamantyl and cycloalkyl having from five to eight carbon atoms. n Said process comprises contacting 4-(2-pyridyl-amidoethyl) piperidine of the structue ##SPC2## n With substantially one equivalent of sulfamide thereby exclusively sulfonating the piperidine nitrogen atom. Said 4-(2-pyridylamidoethyl)piperidines from the corresponding 4-(2-pyridylamidoethyl) pyridines by selectively activating the more basic nitrogen atom of said pyridine compound either by N-alkylation or by contact with acid and then exclusively reducing the activated pyridine ring with either hydrogen alone or in combination with a metal hydride. Said 4-(2-pyridylamidoethyl)pyridines are produced by contacting 4-(2-aminoethyl)pyridine with a pyridyl acid chloride of the formula R(C=O)Cl. The piperidine sulfonamides produced by the process of the instant invention are converted to the desired hypoglycemic agent by methods well-known to those skilled in the art. n The 4-(2-pyridylamidoethyl)pyridines and piperidines of the instant invention are themselves novel compounds useful as intermediates in the synthesis of piperidine sulfamylurea hypoglycemic agents.

专利号:JP-2012530068-A
优先权日:2009-06-12
标题 :Improved synthesis of picoplatin