专利号:US-8735391-B2 优先权日:2008-09-26 标 题 :Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods 发明人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J 权利人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J; UNIV KANSAS 摘要:A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
专利号:US-4388310-A 优先权日:1982-03-01 标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids 发明人:CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.
专利号:US-2005137391-A1 优先权日:1999-02-04 标题 :Process for the synthesis of oligomeric compounds
专利号:US-7186822-B2 优先权日:1999-02-04 标 题 :Process for the synthesis of oligomeric compounds
专利号:US-7199236-B2 优先权日:1999-02-04 标 题 :Process for the synthesis of oligomeric compounds
专利号:US-7227016-B2 优先权日:1999-02-04 标 题 :Process for the synthesis of oligomeric compounds 发明人:RAVIKUMAR VASULINGA T; MANOHARAN MUTHIAH; CAPALDI DANIEL C; KROTZ ACHIM; COLE DOUGLAS L; GUZAEV ANDREI 权利人:ISIS PHARMACEUTICALS INC 摘要:Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.
摘要:Kroon, E.; Zarganes Tzitzikas, T.; Neochoritis, C. G.; Dömling, A., Science of Synthesis: Applications of Domino Transformations in Organic Synthesis, (2015) 2, 428. 摘要:Bagal, D. B.; Bhanage, B. M., Science of Synthesis: Catalytic Reduction in Organic Synthesis, (2018) 2, 387. 摘要:Tang, R.-Y., Science of Synthesis: Knowledge Updates, (2024) 1, 418.