CAS: 87120-72-7; Tert-Butyl 4-Aminopiperidine-1-Carboxylate

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CAS号206273-87-2 4-苄氨基哌啶-1-甲酸叔丁酯 | CAS号79099-07-3 1-B°C-4-哌啶酮 | CAS号150008-24-5 4-肟-1-B°C-哌啶 | CAS号873088-90-5 1,1-dimethyleth... | CAS号13035-19-3 4-氨基哌啶 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号180695-80-1 4-叠氮哌啶-1-羧酸叔丁酯 | CAS号153198-06-2 TERT-BUTYL 4-(2... | CAS号100-52-7 苯甲醛 | CAS号1093759-67-1 4-乙酰氨基哌啶-1-甲酸叔丁酯 | CAS号306934-84-9 4-(4-甲氧基苯胺)四氢-1... | CAS号939986-76-2 4-[(6-氯-4-嘧啶基)氨... | CAS号205058-11-3 4-(2-氧代-5-苯基-1,... | CAS号206274-13-7 4-(环己基氨基)哌啶-1-羧酸叔丁酯 | CAS号301225-40-1 4-(2-嘧啶胺)四氢吡啶羧酸叔丁酯 | CAS号206273-87-2 4-苄氨基哌啶-1-甲酸叔丁酯 | CAS号534595-51-2 1-N-B°C-4-异丙胺哌啶 | CAS号1042224-77-0 4-[(6-溴-2-吡啶基)氨... | CAS号309251-30-7 2-(2-fluorophen...

📜4-氨基-1-苄基哌啶置于palladium Dihydroxide Ammonium Hydroxide,氢气,三乙胺体系中,用 甲醇,二氯甲烷 作为反应溶剂,20.0 °C,344.75 Kpa 条件下,反应 36.0H,反应生成 1-Boc-4-氨基哌啶
参考文献:N-(1-苄基哌啶-4-基)芳基乙酰胺类似物作为有效的sigma1受体配体的合成与构效关系.
标题:N-(1-苄基哌啶-4-基)芳基乙酰胺类似物作为有效的sigma1受体配体的合成与构效关系.
摘要:合成了一系列n-(1-苄基哌啶-4-基)芳基乙酰胺,并评估了它们与sigma1和sigma2受体的结合特性.与先前报道的n-(1-苄基哌啶-4-基)苯基乙酰胺的sigma1 / Sigma2受体结合数据一致,下面报告的所有n-(1-苄基哌啶-4-基)芳基乙酰胺化合物均显示出对sigma1的亲和力高于sigma2受体.用噻吩,萘基或吲哚芳环取代苯乙酰胺部分的苯环对sigma1受体的亲和力没有明显影响.用咪唑或吡啶基芳环取代苯环会导致对sigma1受体的亲和力损失> 60倍,并且对sigma2受体的结合亲和力不明显.苄基芳香环上的取代显示出对sigma1受体的亲和力相似或略有降低.苯乙酰胺部分和苄基上的芳香环都被卤素取代,导致对sigma(1)受体的亲和力相似,并且对sigma2受体的亲和力大大提高.比较分子场分析表明,苯乙酰胺芳环中取代基的静电性质强烈影响与sigma1受体的结合.化合物1,
DOI:10.1021/jm010384J

专利信息

专利号:US-9388147-B2
优先权日:2009-11-13
标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis
发明人：MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN
权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ RL
摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.

专利号:US-8178672-B2
优先权日:2004-10-19
标 题:Synthesis of imidazooxazole and imidazothiazole inhibitors of p38 MAP kinase
发明人：ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC
权利人:ASHWELL MARK A; TANDON MANISH; LAPIERRE JEAN-MARC; ARQULE INC
摘要:An efficient route for the synthesis is of formula (I) of imidazooxazole and imidazothiazole inhibitors of the p38 MAP kinase pathway, useful as therapeutics for disease conditions including inflammation and auto-immune responses is described.

专利号:US-2022274930-A1
优先权日:2019-06-14
标题:Processes and compounds for the decarboxylative amination of redox-active esters with diazirines
发明人：LOPCHUK JUSTIN M; CHANDRACHUD PREETI P
权利人:H LEE MOFFITT CANCER CT & RES
摘要:The invention described herein relates generally to processes for the synthesis of amine-containing organic compounds. More specifically, described herein relates to processes for the decarboxylative amination of redox-active esters with diazirines and the products formed thereof. Compounds for use in the above processes are also described.

专利号:US-2009156465-A1
优先权日:2005-12-30
标题:Derivatives of beta-amino acid as dipeptidyl peptidase-iv inhibitors
发明人：SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND
权利人:SATTIGERI JITENDRA A; AHMED SHAHADAT; ANDAPPAN MURUGAIAH M S; SETHI SACHIN; SHARMA LALIMA; PAL CHANCHAL KUMAR; KANDALKAR SACHIN RAMESH; MAHAJAN DIPAK C; KISHORE KAUSHAL; BHATIA SUMATI; GADHAVE ANIL G; BANSAL VINAY S; DAVIS JOSEPH ALEXANAND
摘要:The present invention relates to β-amino acid derivatives as dipeptidyl peptidase-IV inhibitors and the processes for the synthesis of the same. This invention also relates to pharmacological compositions containing the compounds of the present invention, and methods of treating diabetes, especially type 2 diabetes, as well as prediabetes, diabetic dyslipidemia, metabolic acidosis, ketosis, satiety disorders, and obesity. These inhibitors can also be used to treat conditions manifested by a variety of metabolic, neurological, anti-inflammatory, and autoimmune disorders like inflammatory disease, multiple sclerosis, rheumatoid arthritis; viral, cancer and gastrointestinal disorders. The compounds of this invention can also be used for treatment of infertility arising due to polycystic ovary syndrome.

专利号:US-9890126-B2
优先权日:2012-04-24
标 题:Synthesis of novel inhibitors of isoprenoid biosynthesis (ISPF)
发明人：HAGEN TIMOTHY J; ZHANG ZHENG; LAZOWSKI ZACHARY; CLARE MICHAEL; BEGLEY DARREN W
权利人:UNIV NORTHERN ILLINOIS BOARD OF TRUSTEES; BERYLLIUM DISCOVERY CORP
摘要:Antibacterial and antimalarial IspF inhibitor compounds and compositions are described. Methods include administering described compounds and compositions to treat bacterial or parasitic infections and to inhibit parasite or bacterial growth.

专利号:US-9604985-B2
优先权日:2013-06-10
标 题 :Process for the preparation of chiral tert-butyl 4-((1R,2S,5R)-6(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carb derivatives and (2S,5R)-7-oxo-N-piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide
发明人：MILLER STEVEN P; LIMANTO JOHN; ZHONG YONG-LI; YASUDA NOBUYOSHI; LIU ZHIJIAN
权利人:MERCK SHARP & DOHME
摘要:A process for the preparation of N-protected 6-(piperidin-4-ylcarbamoyl)piperidin-3-yl sulfonates of Formula (III): which comprises contacting a lactone of Formula (II): with an azacycloalkylamine of formula (II-Am): followed by contact with a sulfonyl halide of formula (II-Su): R 4 —SO 2 W (II-Su) in the presence of tertiary amine base, wherein P G1 and P G2 are amine protective groups; k, p and q are 0, 1, or 2, and W, R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 , and R 9 are defined herein. Additional embodiments add a series of process steps leading to the synthesis of 7-oxo-1,6-diazabicyclo[3.2.1]octanes suitable for use as β-lactamase inhibitors.