CAS: 54187-04-1; N-(Dicyclopropylmethyl)-4,5-Dihydrooxazol-2-Amine

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CAS号54187-44-9 N-(dicyclopropy... | CAS号54187-03-0 3-(2-chloroethy...

合成工艺路线路线简述

    1-(2-氯乙基)-3-(二环丙基甲基)脲置于乙醚,氨,水,利美尼啶,1-(2-氯乙基)-3-(二环丙基甲基)脲体系中,用 水 作为反应溶剂,化学反应 2.0H,反应生成 利美尼啶
    参考文献:2-Amino Oxazolines And Process For Making The Same
    标题:2-Amino Oxazolines And Process For Making The Same
    摘要:本发明涉及置换在氮杂环上2位的环丙基甲基胺,以提供新的化合物,其化学式为##str1## 其中a为氧,硫或氮; 一般情况下,其他"r"变量为氢,低烷基,环丙基或低烷基取代的环丙基; N为0至3的数字,包括其酸加成盐.这些化合物是心血管药物,能够抑制中枢神经系统.它们的效果包括催眠,镇痛和神经调节.它们可以用作降压药物.

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    专利信息


    专利号:US-8377406-B1
    优先权日:2012-08-29
    标 题 :Synthesis of bis(fluorosulfonyl)imide
    发明人:SINGH RAJENDRA P; MARTIN JERRY LYNN; POSHUSTA JOSEPH CARL
    权利人:BOULDER IONICS CORP; SINGH RAJENDRA P; MARTIN JERRY LYNN; POSHUSTA JOSEPH CARL
    摘要:The present invention provides methods for producing bis(fluorosulfonyl) compounds of the formula:n nF—S(O) 2 —Z—S(O) 2 —F  In nby contacting a nonfluorohalide compound of the formula:n nX—S(O) 2 —Z—S(O) 2 —Xn nwith bismuth trifluoride under conditions sufficient to produce the bis(fluorosulfonyl) compound of Formula I, where Z and X are those defined herein.

    专利号:US-10391067-B2
    优先权日:2015-08-18
    标题:Prevention and treatment of neurodegenerative diseases through autophagy activity mediated by a synthetic ligand or arginylated BIP binding to the P62 ZZ domain
    发明人:KWON YONG TAE; KIM BO YEON; CHA HYUNJOO; YOO YOUNG DONG; Yu ji-eun
    权利人:SEOUL NAT UNIV R&DB FOUNDATION; KOREA RES INST BIOSCIENCE & BIOTECHNOLOGY; AUTOTAC BIO
    摘要:The pharmacokinetics and key technologies of the present invention are summarized in FIG. 1. Particularly, malignant misfolded proteins such as mutant huntingtin and alpha-synuclein are coagulated and grow into oligomeric coagulum ({circle around (1)}, {circle around (2)}, fibrillar coagulum ({circle around (3)}) and eventually inclusion body ({circle around (4)}). Young neurons produce a large amount of Nt-Arg through N-terminal arginylation ({circle around (5)}) of vesicle chaperones such as BiP secreted into the cytoplasm, and then arginylated BiP (R-BiP) is secreted binds to the misfolded proteins ({circle around (6)}). As a ligand, the Nt-Arg of R-BiP binds to the p62 ZZ domain ({circle around (7)}), and the normally inactivated closed form of p62 is changed to an open form, leading to structural activation ({circle around (8)}). As a result, PB1 and LC3-binding domains are exposed. The PB1 domain induces oligomerization ({circle around (9)}), leading to the concentration as a p62 body ({circle around (10)}) that is a coagulum capable of being degraded by autophagy. Then, p62 binds to LC3, which is protruding from the autopagosomal membranes, leading to the completion of autophagy targeting ({circle around (11)}) and lysosomal proteolysis. Since autophagy proteolysis including steps ({circle around (5)})-({circle around (11)}) is strong in young neurons, cytotoxic protein coagulums ({circle around (1)}-{circle around (5)}) do not accumulate. However in aged neurons, autophagy proteolysis including steps {circle around (5)}-{circle around (11)} is weakened, and protein coagulums ({circle around (1)}-{circle around (5)}) accumulate and become cytotoxic. In this invention, p62 is intentionally activated ({circle around (12)}, {circle around (13)}) by using low mass ligands of the p62 ZZ domain to effectively remove huntingtin and alpha-synuclein protein coagulums. Particularly, in step {circle around (12)}, p62 ligated with a ligand accelerates the oligomerization of p62-R-BiP-misfolded protein ({circle around (9)}) and the formation of autophagy coagulum ({circle around (10)}). In step ({circle around (13)}), the ligand-p62 conjugate acts as an autophagy activator ({circle around (14)}) to induce the synthesis of LC3 and the conversion of LC3-I into LC3-II in order to accelerate the formation of autophagosomes ({circle around (15)}).

    专利号:EP-0846657-B1
    优先权日:1996-12-03
    标题 :Synthesis of phosphorus pentafluoride by fluorination of phosphorus trichloride
    发明人:CHEMINAL BERNARD; JACCAUD MICHEL; JOUBERT PHILIPPE; BONNET PHILIPPE
    权利人:ATOCHEM ELF SA
    摘要:Preparation of phosphorus pentafluoride is carried out in the liquid phase by fluorination of phosphorus trichloride with hydrofluoric acid in the presence of chlorine. Preferably, the HF/PCl3 molar ratio is ≥ 5, especially 6-30, and the Cl2/PCl3 molar ratio is ≥ 1, more preferably 1-1.4, especially 1-1.2. Preferably the process may be carried out in a discontinuous manner by introducing PCl3, HF and Cl2 in this order into a low temperature reactor, stirring the reaction mixture until the pressure is constant, gradually reducing the reactor pressure and then separating the reaction products.

    专利号:JP-H10245211-A
    优先权日:1996-12-03
    标题:Synthesis of phosphorus pentafluoride by fluorination of phosphorus trichloride

    专利号:EP-0712826-A1
    优先权日:1994-11-17
    标题:1,1,1-Trifluoroethane synthesis using a supported lewis acid
    发明人:ELSHEIKH MAHER YOUSEF; BOLMER MICHAEL SHEPPARD
    权利人:ATOCHEM NORTH AMERICA ELF
    摘要:Process for synthesizing 1,1,1-trifluoroethane (143a) in the gaseous phase by reacting 1,1-difluoro-1-chloroethane in gaseous phase in the presence of a catalyst selected from the SbV, TiIV,and SnIV salts. The process may be run without co-feeding chlorine gas as a coactivator, in the presence or absence of an impurity selected from HCl and 141b. The catalyst may be unsupported or supported on activated carbon. The formation of olefin byproduct was not detected when the process of the invention was conducted under the conditions described.

    专利号:US-5116592-A
    优先权日:1986-06-02
    标题:Fluorinated carbons and uses thereof
    发明人:WEINBERG NORMAN L
    权利人:ELECTROSYNTHESIS CO INC
    摘要:Specifically fluorinated carbons have enhanced chemical and/or electrochemical stabilities to corrosion, improved hydrophobicity, lubricating properties, etc., making them especially useful as electrodes in both energy consuming and energy producing electrochemical cells, such as batteries, fuel cells and cells for the electrochemical synthesis of organic and inorganic chemical compounds. The specifically fluorinated carbons may also be employed as lubricants, in fabrication of reactors for generating energy, chemical reaction vessels and as catalyst supports.
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    主要参考文献


    1: Perera ND, Sheean RK, Lau CL, Shin YS, Beart PM, Horne MK, Turner BJ. Rilmenidine promotes MTOR-independent autophagy in the mutant SOD1 mouse model of amyotrophic lateral sclerosis without slowing disease progression. Autophagy. 2018;14(3):534-551. doi: 10.1080/15548627.2017.1385674. Epub 2017 Dec 17.
    2: Rubinsztein DC, Bento CF, Deretic V. Therapeutic targeting of autophagy in neurodegenerative and infectious diseases. J Exp Med. 2015 Jun 29;212(7):979-90. doi: 10.1084/jem.20150956. Epub 2015 Jun 22. Review.
    3: Lim K, Jackson KL, Burke SL, Head GA. The Effects of Rilmenidine and Perindopril on Arousal Blood Pressure during 24 Hour Recordings in SHR. PLoS One. 2016 Dec 21;11(12):e0168425. doi: 10.1371/journal.pone.0168425. eCollection 2016.

    合成参考文献


    摘要:S76 | LUXPHARMA | Pharmaceuticals Marketed in Luxembourg | Pharmaceuticals marketed in Luxembourg, as published by d'Gesondheetskeess (CNS, la caisse nationale de sante, www.cns.lu), mapped by name to structures using CompTox by R. Singh et al. (2021) DOI:10.1021/acsenvironau.1c00008. List downloaded from
    参考文献:10.1111/j.1472-8206.1996.tb00589.x
    摘要:Marsault R, Taddei S, Boulanger C, Illiano S, Vanhoutte P. Rilmenidine activates postjunctional alpha1‐ and alpha2‐adrenoceptors in the canine saphenous vein. Fundamemntal Clinical Pharma. 1996 Jul 08;10(4):379–86. doi: 10.1111/j.1472-8206.1996.tb00589.x.
    摘要:van Zwieten PA. From alpha and beta to I1: an overview of sympathetic receptors involved in blood pressure control targets for drug treatment. J Cardiovasc Pharmacol. 1996;27 Suppl 3():S5–10.
    摘要:Drzewoski J, Wiśniewska-Jarosińska M. [Clinical pharmacology of hypotensive drugs acting on central imidazoline receptors]. Pol Arch Med Wewn. 1998 Dec;100(6):561–9.
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