CAS: 161975-39-9; Tert-Butyl 4-(((Methylsulfonyl)Oxy)Methyl)Piperidine-1-Carboxylate

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CAS号124-63-0 甲基磺酰氯 | CAS号123855-51-6 N-B°C-4-哌啶甲醇 | CAS号7143-01-3 甲基磺酸酐 | CAS号24424-99-5 二碳酸二叔丁酯 | CAS号6457-49-4 4-哌啶甲醇 | CAS号84358-13-4 1-B°C-4-哌啶甲酸 | CAS号498-94-2 4-哌啶甲酸 | CAS号145508-94-7 1-叔丁氧羰基-4-碘甲基哌啶 | CAS号144222-22-0 1-B°C-4-(氨基甲基)哌啶 | CAS号256411-39-9 1-B°C-4-(氰基甲基)哌啶 | CAS号176967-62-7 4-(Piperidin-4-... | CAS号917903-78-7 3-(4-哌啶基甲氧基)苯甲酸甲酯

N-Boc-4-哌啶甲酸乙酯置于lithium Aluminium Tetrahydride,三乙胺体系中,用 四氢呋喃,二氯甲烷 用作溶剂,化学反应 16.0H,反应生成1-Boc-4-甲磺酰基氧甲基哌啶
参考文献:Polyfluorinated Compounds Acting As Bruton Tyrosine Kinase Inhibitors
标题:Polyfluorinated Compounds Acting As Bruton Tyrosine Kinase Inhibitors
摘要:本文描述了一种新型的多氟取代吡唑嘧啶化合物或其盐.这些化合物是布鲁顿酪氨酸激酶(btk)抑制剂.这些化合物可能具有更好的btk抑制选择性和药代动力学特性.本文披露了这些化合物的合成方法.本文还披露了多氟取代苯甲酮和取代苯氧基苯的新型合成方法.还披露了包括上述btk抑制剂的药物组合物.本发明还涉及包含上述化合物作为活性成分的药物配方.本发明还包括通过给予btk抑制剂及其配方来治疗和抑制自身免疫疾病,过敏性疾病,炎症性疾病和癌症的治疗方法.

专利信息

专利号:EP-3091007-A1
优先权日:2015-05-08
标 题 :Process for the preparation of piperidine compounds
发明人：ATTOLINO EMANUELE; RIZZO ELISABETH; ROSSI DAVIDE
权利人:DIPHARMA FRANCIS SRL
摘要:The present invention relates to a process for the preparation of intermediates useful in the synthesis of efinaconazole and their use in the synthesis of efinaconazole.

专利号:US-2023192718-A1
优先权日:2018-03-30
标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof
发明人：SANDANAYAKA VINCENT
权利人:NIROGY THERAPEUTICS INC
摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.

专利号:US-7645754-B2
优先权日:2001-12-20
标题 :Pyrrolopyrimidine A2B selective antagonist compounds, their synthesis and use
发明人：CASTELHANO ARLINDO; MCKIBBEN BRYAN; STEINIG ARNO
权利人:OSI PHARM INC
摘要:The subject invention provides compounds having the structure: n n n n n n n n n n n n wherein,n R 1 is a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O) R a ; R 2 is hydrogen or a substituted or unsubstituted alkyl, wherein the substituent is hydroxyl, dihydroxy, carboxyl, —C(â•?O)NR a R b , —NR a R b , —NR a C(â•?O)NR a R b , —NR a C(â•?O)OR a , —OC(â•?O)NR a R b , or —NHC(â•?O)R a , or R 1 , R 2 and N together form a substituted piperazine, substituted azetidine ring, or a pyrrolidine ring substituted with —(CH 2 ) 2 OH or —CH 2 C(â•?O)OH; R 3 is a substituted or unsubstituted phenyl or a 5-6 membered heteroaryl ring, wherein the substituent is halogen, hydroxyl, cyano, (C 1 -C 15 )alkyl, (C 1 -C 15 )alkoxy, or —NR a R b ; R 4 is hydrogen or substituted or unsubstituted (C 1 -C 15 )alkyl; R 5 is —(CH 2 ) m OR 6 , —CHNOR 7 , —C(â•?O)NR 8 R 9 , —(CH 2 ) m C(â•?O)OR 10 , —(CH 2 ) k C(â•?O)NR 11 R 12 ;n wherein R 6 is a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or 4-8 membered heterocyclic ring; R 7 is hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl; R 8 and R 9 are each independently hydrogen, or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 1 -C 30 )alkylaryl, (C 1 -C 30 )alkylamino, (C 1 -C 30 )alkoxy, or a saturated or unsaturated, monocyclic or bicyclic, carbocyclic or heterocyclic ring, or R 8 , N, and R 9 together form a substituted or unsubstituted 4-8 membered heterocyclic ring; R 10 is hydrogen or a substituted or unsubstituted (C 1 -C 30 )alkyl, (C 3 -C 10 )cycloalkyl, or an aryl, heteroaryl or heterocyclic ring; R 11 , N and R 12 together form a 4-8 membered heterocyclic ring; R a and R b are each independently hydrogen or alkyl; m is 0, 1, 2 or 3; and k is 1, 2 or 3,n nor a specific enantiomer thereof, or a specific tautomer thereof, or a pharmaceutically acceptable salt thereof, and a method for treating a disease associated with the A 2b adenosine receptor in a sbject in need of such treatment comprising administering to the subject a therapeutically effective amount of the compounds of the invention.

专利号:US-9861636-B2
优先权日:2014-04-29
标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors
发明人：HE WEI
权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD
摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.

专利号:US-2010234603-A1
优先权日:2009-03-13
标题:Process for Making Substituted Aryl Sulfone Intermediates
发明人：LINGHU XIN; LINN KATHLEEN; MALONEY KEVIN M; MCLAUGHLIN MARK; QIAN GANG
权利人:LINGHU XIN; LINN KATHLEEN; MALONEY KEVIN M; MCLAUGHLIN MARK; QIAN GANG
摘要:The present invention relates to novel substituted aryl sulfone intermediates and processes for preparing the same. An aspect of this invention relates to a process for making substituted aryl sulfone intermediates utilizing a one-pot deacylation-carbon/sulfur bond formation step. The invention also relates to a process for preparing intermediates that are used to make the compounds of formula I. Some of the advantages of the present invention include manufacturing flexibility and efficiency, high yield synthesis using a one pot deacylation and carbon-sulfur bond formation step of a thioester intermediate and the like. This and other aspects of the invention will be realized upon review of the specification as a whole.

专利号:US-2010234604-A1
优先权日:2009-03-13
标题:Process for Making Substituted Aryl Sulfone Intermediates
发明人：LINGHU XIN; LINN KATHLEEN; MALONEY KEVIN M; MCLAUGHLIN MARK; QIAN GANG
权利人:LINGHU XIN; LINN KATHLEEN; MALONEY KEVIN M; MCLAUGHLIN MARK; QIAN GANG
摘要:The present invention relates to novel substituted aryl sulfone intermediates and processes for preparing the same. An aspect of this invention relates to a process for making substituted aryl sulfone intermediates utilizing a one-pot deacylation-carbon/sulfur bond formation step. The invention also relates to a process for preparing intermediates that are used to make the compounds of formula I. Some of the advantages of the present invention include manufacturing flexibility and efficiency, high yield synthesis using a one pot deacylation and carbon-sulfur bond formation step of a thioester intermediate and the like. This and other aspects of the invention will be realized upon review of the specification as a whole.