专利号:US-7939679-B2 优先权日:2006-01-19 标题:Method for synthesis of ciguatoxin CTX1B and compounds useful for the synthesis of ciguatoxin CTX1B 发明人:HIRAMA MASAHIRO; INOUE MASAYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Disclosed is a method for total synthesis of CTX1B, which is developed for the synthesis of a ciguatoxin analogue such as CTX3C and enables the more efficient application of an established reaction to the total synthesis of CTC1B. More specifically, disclosed is a method for total synthesis of CTX1B comprising; an O.S-acetal formation for synthesizing a novel compound (3); a radical cyclization reaction for constructing a 9-membered ring formation reaction including a novel compound (6) through a novel compound (8) and yielding a compound (D); and a deprotection for yielding CTX1B. Also disclosed are novel compounds (1) to (8) which are particularly useful for synthesis of CTX1B and can be used for the synthesis of a ciguatoxin analogue.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
专利号:WO-2012047907-A9 优先权日:2010-10-04 标题 :Synthesis of c5-substituted tetracyclines, uses thereof, and intermediates thereto 发明人:MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 权利人:HARVARD COLLEGE; MYERS ANDREW G; WRIGHT PETER M; HECKER EVAN 摘要:The tetracycline class of antibiotics has played a major role in the treatment of infectious diseases for the past 50 years. However, the increased use of the tetracyclines in human and veterinary medicine has led to resistance among many organisms previously susceptible to tetracycline antibiotics. The recent development of a modular synthesis of tetracycline analogs through a chiral enone intermediate has allowed for the efficient synthesis of novel tetracycline analogs never prepared before. The present invention provides more efficient routes for preparing the enone intermediate and allows for a wide variety of substituents at position 5 of the tetracycline ring system.
专利号:US-8269001-B2 优先权日:2005-10-05 标题 :Process for the synthesis of HMG-CoA reductase inhibitors 发明人:CASAR ZDENKO 权利人:CASAR ZDENKO; LEK PHARMACEUTICALS 摘要:A novel synthesis of statins uses Wittig reaction of a heterocyclic core of statin with a lactonized side chain already possessing needed stereochemistry. Any separation of diastereoisomers is performed early in the course of synthesis.
专利号:US-4354972-A 优先权日:1981-06-29 标 题 :Synthesis of steroids 发明人:KAISER EMIL T 权利人:KAISER EMIL T 摘要:This invention relates to the synthesis of steroids which are useful for their biological activity or which may be converted to steroids which have such activity. These syntheses include the steroid compounds and processes for their preparation. n An object of the invention is to provide syntheses which are applicable to materials which are readily available in good supply for converting such materials to steroids which are useful and desirable in the manufacture of pharmaceutical products. n More particularly, I have sought to discover processes and intermediate compounds useful in the synthesis of 24, 25-dihydroxycholesterol from hyodeoxycholic acid or lithocholic acid which are constituents of, and readily available from, animal bile.
专利号:WO-2024182268-A1 优先权日:2023-02-27 标 题 :Liquid phase peptide support synthesis of peptides and peptidomimetics 发明人:HAN AMY 权利人:REGENERON PHARMA 摘要:The present invention provides compounds useful as support for liquid phase organic synthesis e.g., liquid phase organic synthesis of peptides and peptidomimetics. In one aspect, the present invention provides a compound having a structure of Formula (I) where R1, R2, R3, m, and n are as described herein and methods of making and using same.