专利号:WO-9419366-A1 优先权日:1993-02-26 标题 :Chemical synthesis of squalamine 发明人:MORIARTY ROBERT M; GUO LIANG; TULADHAR SUDERSAN M 权利人:MAGAININ PHARMA 摘要:Methods for the chemical preparation or synthesis of the sterol antibiotic squalamine. Preferably, the preparation is by modifying the 3-position of a 3-oxo-7α-hydroxy-24z-ether protected alcohol group-5α-cholestane with a spermidino moiety to form a 3β-spermidino-7α-hydroxy-24z-ether protected group -5α-cholestane; deprotecting the 24-position of the 3β-spermidino-7α-hydroxy-24z-ether protected group-5α-cholestane to the free hydroxyl; and sulfating the 24-position of the 3β-spermidino-7α, 24-dihydroxy-5α-cholestane.
专利号:WO-2024174285-A1 优先权日:2023-02-21 标题:Method for preparing halogenated compound from metal halide salt on basis of mobile phase 发明人:SU REN; Ye Jiani 权利人:UNIV SOOCHOW 摘要:Disclosed is a method for preparing a halogenated compound from a metal halide salt on the basis of a mobile phase. The method comprises: converting an aromatic hydrocarbon, alkane or nitrile compound into a halogenated compound by means of a cheap metal halide salt and a photocatalyst under illumination. The method uses a cheap and safe halide salt as a halogen source, does not introduce additional elemental halogen or an additional oxidant, can implement a reaction at normal temperature and normal pressure, is high in terms of selectivity and friendly to environment, and can be used for replacing an existing synthesis reaction system for halogenated compounds. A mobile phase device is used to replace a tank reactor, such that operation is easy and convenient, the price is low, the substrate adaptability is high, the continuous synthesis of halogenated compounds can be achieved, and the method is suitable for industrial large-scale production.
专利号:US-8506927-B2 优先权日:2011-01-05 标 题 :Pegylated fluorobenzamide analogues, their synthesis and use in diagnostic imaging 发明人:MACH ROBERT H; TU ZHUDE 权利人:MACH ROBERT H; TU ZHUDE; UNIV WASHINGTON 摘要:Pegylated fluoroalkoxybenzamide compounds which selectively bind Sigma-2 receptors are disclosed. These compounds, when labeled with a positron-emitting radioisotope such as 18 F, can be used as radiotracers for medical imaging such as imaging of tumors by positron emission tomography (PET). In addition, these compounds, when labeled with 123 I, can be used as radiotracers for imaging of tumors by single photon emission computed tomography (SPECT). Methods for synthesis of these compounds are also disclosed.
专利号:EP-0468457-B1 优先权日:1990-07-24 标题 :Novel substituted piperidines and their use as inhibitors of cholesterol synthesis 发明人:MCCARTHY JAMES R; BARNEY CHARLOTTE L; WANNAMAKER MARION W 权利人:MERRELL DOW PHARMA 摘要:The present invention relates to a group of compounds which are novel substituted piperidines and which act to inhibit the synthesis of cholesterol in mammals and in fungi.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-2004116724-A1 优先权日:1996-12-06 标 题:Stereoselective synthesis of 24-hydroxylated compounds useful for the preparation of aminosterols, vitamin D analogs, and other compounds 发明人:KINNEY WILLIAM A; JONES STEVEN; ZHANG XUEHAI; RAO MEENA N; BULLIARD MICHEL; MECKLER HAROLD; LEE NANCY 摘要:A method is described for stereoselectively reducing an unsaturated alkyl ketone substituent attached to a fused ring base. In this method, the unsaturated alkyl ketone reacts with a chiral oxazaborolidine reagent. This reaction stereoselectively reduces the unsaturated alkyl ketone to an unsaturated alkyl alcohol. The unsaturated alkyl alcohol can be further reduced, if desired, to produce a saturated alkyl alcohol. The fused ring base can be, for example, a steroid ring base or a base of a vitamin D analog. The process in accordance with the invention can be used with an alkeneone substituent (e.g., a 22-ene-24-one substituent) or an alkyneone substituent (e.g., a 22-yne-24-one substituent) on a steroid ring base to make squalamine or other useful aminosterol compounds and intermediates for making aminosterol compounds.
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