CAS: 53179-11-6; Loperamide

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CAS号39512-49-7 4-(4-氯苯基)-4-羟基哌啶 | CAS号37743-18-3 3,3-二苯基四氢呋喃-2-亚... | CAS号37742-98-6 4-溴-2,2-二苯基丁酸 | CAS号956-89-8 α,α-二苯基-γ-丁内酯

Loperamide Oxide置于sodium Tetrahydroborate体系中,用 乙醇,水 作为反应溶剂,以95%的收率获得产物洛哌丁胺
参考文献:A Chemoselective Deoxygenation Of N-Oxides By Sodium Borohydride-raney Nickel In Water
标题:A Chemoselective Deoxygenation Of N-Oxides By Sodium Borohydride-raney Nickel In Water
摘要:A Simple And Convenient Protocol For Deoxygenation Of Aliphatic And Aromatic N-Oxides To The Corresponding Amines In Good To Excellent Yield Using Sodium Borohydride-Raney Nickel In Water Is Reported. Other Functional Moieties Such As Alkenes,Halides,Ethers,And Amides Are Unaffected Under The Present Reaction Condition. (C) 2010 Elsevier Ltd. All Rights Reserved.
DOI:10.1016/j.Tetlet.2010.08.045

专利信息

专利号:US-9597327-B2
优先权日:2005-05-25
标 题:Synthesis of (R)-N-methylnaltrexone
发明人：DOSHAN HAROLD D; PEREZ JULIO
权利人:PROGENICS PHARM INC
摘要:This invention relates to stereoselective synthesis of R-MNTX and intermediates thereof, pharmaceutical preparations comprising R-MNTX or intermediates thereof and methods for their use.

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-5712269-A
优先权日:1993-04-05
标题 :M2 receptor ligand for the treatment of neurological disorders
发明人：MCCABE R TYLER; WILSON BRYAN R; RHODES CHRISTOPHER A
权利人:PHARMACEUTICAL DISCOVERY CORP
摘要:Muscarinic M2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.

专利号:US-9604987-B2
优先权日:2011-03-23
标题 :Synthesis of autophagy inducing compound and the uses thereof
发明人：LI MIN; Liu liang feng; SONG JU XIAN; Zhang hong jie
权利人:UNIV HONG KONG BAPTIST UNIV
摘要:The present invention relates to a composition comprising compound of formula CB6 or CB8, n nthe pharmaceutically-acceptable carrier, solvent, the salts thereof or a combination thereof which is used to treat autophagy-associated diseases such as Alzheimer's disease, Parkinson's disease, Huntington's disease, etc. The present invention also relates to a method of treating these diseases by administering a therapeutically-effective amount of the compound to the subject in need of the treatment. The present invention further relates to the use of this compound in preparation of the composition to treat the diseases.

专利号:US-9187408-B2
优先权日:2008-10-27
标 题 :Process for the preparation of protected L-alanine derivatives
发明人：ANZALONE LUIGI; FEIBUSH PENINA; VILLANI FRANK J
权利人:JANSSEN PHARMACEUTICA NV; JANSSEN PHARMACEUTICA NV
摘要:The present invention is directed to a novel process for the preparation of protected L-alanine derivatives, useful as intermediates in the synthesis of compounds useful as mu/delta opioid modulators.

专利号:US-6187756-B1
优先权日:1996-09-05
标 题 :Composition and methods for treatment of neurological disorders and neurodegenerative diseases
发明人：LEE ROBERT K K; WURTMAN RICHARD J
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:It has been discovered that the stimulation of β-adrenergic receptors, which activate cAMP formation, give rise to increased APP and GFAP synthesis in astrocytes. Hence, the in vitro or in vivo exposure of neuronal cells to certain compositions comprising β-adrenergic receptor ligands or agonists, including, e.g., norepinephrine, isoproterenol and the like, increases APP mRNA transcription and consequent APP overproduction. These increases are blocked by β-adrenergic receptor antagonists, such as propranolol. The in vitro or in vivo treatment of these cells with 8Br-cAMP, prostaglandin E 2 (PG E 2 ), forskolin, and nicotine ditartrate also increased APP synthesis, including an increase in mRNA and holoprotein levels, as well as an increase in the expression of glial fibrillary acidic protein (GFAP). Compositions and methods are disclosed of regulating APP overexpression and mediating reactive astrogliosis through cAMP signaling or the activation of β-adrenergic receptors. It has further been found that the increase in APP synthesis caused by 8Br-cAMP, PG E 2 , forskolin, or nicotine ditartrate is inhibited by immunosuppressants or anti-inflammatory agents, such as cyclosporin A, and FK-506 (tacrolimus), as well as ion-channel modulators, including ion chelating agents such as EGTA, or calcium/calmodulin kinase inhibitors, such as KN93. The present invention has broad implications in the alleviation, treatment, or prevention of neurological disorders and neurodegenerative diseases, including Alzheimer's Disease.