CAS: 129432-25-3; 2,6-Dichloro-4-Methylpyridin-3-Amine

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CAS号38841-54-2 2,6-二氯-4-甲基烟酰胺 | CAS号875-35-4 2,6-二氯-4-甲基-3-吡啶氰 | CAS号3430-27-1 3-氨基-4-甲基吡啶 | CAS号142266-58-8 2-chloro-N-(2,6...

3-氰基-4-甲基-2,6-二氯吡啶置于sodium Hydroxide,硫酸,溴体系中,化学反应生成2,6-二氯-4-甲基-3-氨基吡啶
参考文献:Novel Non-Nucleoside Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones As Potent Inhibitors Of Both Wild-Type And Cysteine-181 Hiv-1 Reverse Transcriptase Enzymes
标题:Novel Non-Nucleoside Inhibitors Of Human Immunodeficiency Virus Type 1 (Hiv-1) Reverse Transcriptase. 4. 2-Substituted Dipyridodiazepinones As Potent Inhibitors Of Both Wild-Type And Cysteine-181 Hiv-1 Reverse Transcriptase Enzymes
摘要:The Major Cause Of Viral Resistance To The Potent Human Immunodeficiency Virus Type 1 Reverse Transcriptase (Rt) Inhibitor Nevirapine Is The Mutation Substituting Cysteine For Tyrosine-181 In Rt (Y181C Rt),An Evaluation,Against Y181C Rt,Of Previously Described Analogs Of Nevirapine Revealed That The 2-Chlorodipyridodiazepinone 16 Is An Effective Inhibitor Of This Mutant Enzyme. The Detailed Examination Of The Structure-Activity Relationship Of 2-Substituted Dipyridodiazepinones Presented Below Shows That Combined Activity Against The Wildtype And Y181C Enzymes Is Achieved With Aryl Substituents At The 2-Position Of The Tricyclic Ring System. In Addition,The Substitution Pattern At C-4,N-5,And N-11 Of The Dipyridodiazepinone Ring System Optimum For Inhibition Of Both Wild-Type And Y181C Rt Is No Longer The 4-Methyl-11-Cyclopropyl Substitution Preferred Against The Wild-Type Enzyme But Rather The 5-Methyl-11-Ethyl (Or 11-Cyclopropyl) Pattern. The More Potent 8-Substituted Dipyridodiazepinones Were Evaluated Against Mutant Rt Enzymes (L100I Rt,K103N Rt,P236L Rt,And E138K Rt) That Confer Resistance To Other Non-Nucleoside Rt Inhibitors,And Compounds 42,62,And 67,With Pyrrolyl,Aminophenyl,And Aminopyridyl Substituents,Respectively,At The 2-Position,Were Found To Be Effective Inhibitors Of These Mutant Enzymes Also.
Doi:10.1021/jm00024A010

专利信息

专利号:US-6111112-A
优先权日:1999-01-22
标题 :Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone
发明人：GROZINGER KARL
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:A method for making 3-amino-2-chloro-4-methylpyridine from malononitrile, as depicted in the following reaction scheme. ##STR1##

专利号:US-6136982-A
优先权日:1999-01-22
标 题:Synthesis of 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate
发明人：GROZINGER KARL
权利人:BOEHRINGER INGELHEIM PHARMA
摘要:A method for making 3-amino-2-chloro-4-methylpyridine from acetone and ethyl cyanoacetate, as depicted in the following reaction scheme. ##STR1##

专利号:WO-0043365-A1
优先权日:1999-01-22
标 题:Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone

专利号:EP-1064265-A1
优先权日:1999-01-22
标 题 :Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone

专利号:JP-2002535311-A
优先权日:1999-01-22
标 题 :Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone

专利号:EP-1064265-B1
优先权日:1999-01-22
标 题 :Synthesis of 3-amino-2-chloro-4-methylpyridine from malononitrile and acetone