专利号:US-2003182068-A1 优先权日:2001-10-30 标 题 :Device and methods for directed synthesis of chemical libraries 发明人:BATTERSBY BRONWYN J; MILLER CHRISTOPHER R; TRAU MATHIAS; WAY JEFFERY C; JOHNSTON ANGUS 摘要:The invention features a sort computer which interfaces with a sorting device in order to control the sorting of beads on a bead by bead basis. The invention further features novel methods for the directed synthesis of encoded libraries of oligomers, e.g., oligonucleotides, on beads. These methods allow the synthesis of libraries that are sufficiently large to permit complex genomic analyses to be carried out. New methods of using the encoded libraries also are described.
专利号:US-6998484-B2 优先权日:2000-10-04 标 题:Synthesis of purine locked nucleic acid analogues 发明人:KOCH TROELS; JENSEN FLEMMING REISSIG 权利人:SANTARIS PHARMA AS 摘要:The present invention relates to a new method for the synthesis of purine LNA (Locked Nucleic Acid) analogues which provides a higher overall yield. The method comprising a regioselective 9-N purine glycosylation reaction followed by a one-pot nucleophilic aromatic substitution reaction of the 6-substituent in the purine ring and simultaneous nucleophile-induced intramolecular ring closure of the C-branched carbohydrate to form novel purine LNA analogues. The novel strategy is illustrated by the synthesis of the novel compound (1S,3R,4R,7S)-7-benzyloxy-1-methanesulfonylmethyl-3-(guanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane which is easily converted into (1S,3R,4R,7S)-7-hydroxy-1-hydroxymethyl-3-((2-N-isobutyrylguanin-9-yl)-2,5-dioxabicyclo[2.2.1]heptane after isobutyryl protection of the 2-amino purine group and subsequent substitution of 1-methanesulfonyl with benzoate, debenzoylation and debenzylation.
专利号:US-9440940-B2 优先权日:2014-03-18 标 题:Methods for synthesis of psoralen derivatives 发明人:REFOUVELET BERNARD 权利人:MACOPHARMA S A S 摘要:Methods for the synthesis of psoralen derivatives are provided. In one embodiment, the method may include acetylating a compound of formula (II) to form a compound of formula (III), subjecting the compound of formula (III) to a Fries rearrangement to form a compound of formula (IV), and subjecting the compound of formula (IV) to cyclization, reduction and aromatization, to form a compound having the following formula (I):
专利号:US-5247099-A 优先权日:1989-08-17 标题:Process for synthesis of 7-hydroxy coumarins having substitutions in the 4-position 发明人:CELEBUSKI JOSEPH E 权利人:ABBOTT LAB 摘要:A process for synthesis of a compound of the formula: said process comprising the steps of (a) reacting 4-bromomethyl-7-methoxy coumarin with a malonic ester under conditions sufficient to achieve condensation of the ester to give the monoalkylated (2-bis(carbalkoxy)-2-R1-1-ethyl) derivative; (b) removing one of the carbalkoxy groups from the product of step (a); (c) demethylation of the product of step (b) to give the 7-hydroxycoumarin compound; and (d) chemically modifying the remaining ester to yield a desired R2.
专利号:US-7598291-B2 优先权日:2004-09-02 标题 :Methods and compositions for enhancing collagen and proteoglycan synthesis in the skin 发明人:NIMNI MARCEL; HAN BO 权利人:NIMNI MARCEL; HAN BO 摘要:A composition for application to the skin can stimulate the in vivo synthesis of collagen and proteoglycans and improve the appearance of the skin, increasing its elasticity and fullness. In general, a composition according to the present invention comprises: (1) an antioxidant compound in a quantity sufficient to enhance collagen synthesis in the skin; (2) an organic penetrant in which the antioxidant compound is soluble in a sufficient quantity that a concentration of the antioxidant compound sufficient to enhance collagen synthesis can be applied topically and penetrate the skin; (3) a mixture of essential amino acids; (4) a supplemental source of sulfur; and (5) a topical pharmaceutically acceptable carrier. The antioxidant compound can be lipoic acid, a lipoic acid analogue or derivative, a bioflavonoid, a constituent of ginkgo, or an isoflavone. The organic penetrant is preferably benzyl alcohol. Other ingredients, such as esters of tocopherol and ascorbic acid, can be included.
专利号:US-5679773-A 优先权日:1995-01-17 标题 :Reagants and methods for immobilized polymer synthesis and display 发明人:HOLMES CHRISTOPHER P 权利人:AFFYMAX TECH NV 摘要:Compounds and methods for solid phase synthesis of organic molecules including peptides, oligonucleotides, benzodiazepines, beta -turn mimetics, and prostaglandins. The present invention provides new reagents in the form of linking groups and resins and substrates having attached linking groups which are useful in solid phase synthesis of high density arrays of organic molecules. The invention also provides methods which increase yields of various organic synthesis strategies.
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合成参考文献
参考文献:10.1107/s1600536810029430 摘要:Adfa M, Koketsu M, Ebihara M. 6-Benzyl-oxycoumarin. Acta Crystallogr Sect E Struct Rep Online. 2010 Jul 31;66(Pt 8):o2190. 参考文献:10.1007/s10886-011-9968-6 摘要:Adfa M, Hattori Y, Yoshimura T, Komura K, Koketsu M. Antifeedant and Termiticidal Activities of 6-Alkoxycoumarins and Related Analogs Against Coptotermes formosanus Shiraki. Journal of Chemical Ecology. 2011 May 20;37(6):598–606. doi: 10.1007/s10886-011-9968-6.