CAS: 132449-46-8; 2-(4-(4-(4-Chloro-1H-Pyrazol-1-yl)Butyl)Piperazin-1-yl)Pyrimidine

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2-[4-(4-Bromobutyl)-1-Piperazinyl]-Pyrimidine 87789-48-8

📜4-氯吡唑,丁螺环酮ep杂质b置于4-氯吡唑体系中,用87的收率获得来索吡琼
参考文献:Process For The Preparation Of Aryl (Or Heteroaryl)
标题:Process For The Preparation Of Aryl (Or Heteroaryl)
摘要:本发明涉及一种制备芳基(或杂环芳基)哌嗪基丁唑衍生物的过程,其对应于一般式i,其中ar表示从不同取代的芳基,不同取代的2-嘧啶基,2-N-甲基咪唑和3-(1,2-苯并异噻唑)中选择的氮或其他芳基基团.Z.Sub.1表示氮原子或可选择用c-R.Sub.1表示的可选取代碳原子,Z.Sub.2表示氮原子或可选择用c-R.Sub.2表示的可选取代碳原子,Z.Sub.4表示氮原子或可选择用c-R.Sub.4表示的可选取代碳原子,R.Sub.1,R.Sub.2,R.Sub.3和r.Sub.4相同或不同,也可以是另一个环的一部分,芳香或其他,表示氢原子,卤素,低碳基,硝基,羟基,烷氧基,氰基,羧基,羧酰胺基,烷基羧酸酯基,芳基或取代芳基基团,磺酸基,磺酰胺基,在氨基上可选择取代的氨基或取代氨基基团,其中##str2##中ar具有上述所述的含义,X表示卤素原子,与一般式iii的化合物反应.其中一般式iii为##str3##其中z.Sub.1,Z.Sub.2,Z.Sub.4和r.Sub.3具有上述所述的含义.

专利信息

专利号:US-7309799-B2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof
发明人：BUCHWALD STEPHEN L; SWAGER TIMOTHY M; RARIY ROMAN V
权利人:COLLEGIUM PHARMACEUTICAL INC
摘要:One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

专利号:US-7749985-B2
优先权日:2006-09-15
标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use
发明人：GALLOP MARK A; XU FENG; PHAN THU; DILIP USHA; PENG GE
权利人:XENOPORT INC
摘要:Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of making acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, methods of using acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, and pharmaceutical compositions comprising acyloxyalkyl carbamate prodrugs 3-aminopropylphosphinic acid and analogs thereof for treating diseases or disorders such as mild cognitive impairment, cognitive impairment associated with Alzheimer's disease Alzheimer's disease, depression, anxiety, and epilepsy are disclosed. Acyloxyalkyl carbamate prodrugs of 3-aminopropylphosphinic acid and analogs thereof, which are suitable for oral administration and sustained release oral dosage forms are also disclosed.

专利号:US-2005282898-A1
优先权日:2004-06-01
标 题 :Methods for the synthesis of milnacipran and congeners thereof

专利号:WO-2005118564-A2
优先权日:2004-06-01
标 题:Methods for the synthesis of milnacipran and congeners thereof

专利号:US-2008146526-A1
优先权日:2006-09-15
标 题 :Acyloxyalkyl carbamate prodrugs, methods of synthesis and use

专利号:US-2009286759-A1
优先权日:2006-09-15
标题:Acyloxyalkyl carbamate prodrugs, methods of synthesis and use