专利号:US-9884830-B2 优先权日:2004-05-21 标题 :Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; CHAREST MARK G; LERNER CHRISTIAN D; BRUBAKER JASON D; SIEGEL DIONICIO R 权利人:HARVARD COLLEGE 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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetracycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-proliferative agents in the treatment of diseases of humans or other animals.
专利号:US-8486921-B2 优先权日:2006-04-07 标 题:Synthesis of tetracyclines and analogues thereof 发明人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU 权利人:MYERS ANDREW G; BRUBAKER JASON D; SUN CUIXIANG; WANG QIU; HARVARD COLLEGE 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 modular synthesis of tetracyclines and tetracycline analogs described provides an efficient and enantioselective route to a variety of tetracycline analogs and polycyclines previously inaccessible via earlier tetra-cycline syntheses and semi-synthetic methods. These analogs may be used as anti-microbial agents or anti-pro liferative agents in the treatment of diseases of humans or other animals.
专利号:WO-2024262824-A1 优先权日:2023-06-20 标 题 :Novel process for synthesis of polysubstituted pyridine derivatives 发明人:PARK SEUNG BUM; YI SIHYEONG 权利人:SEOUL NAT UNIV R&DB FOUNDATION 摘要:The present invention relates to a novel method for synthesizing a polysubstituted pyridine derivative and, more specifically, to a method for synthesizing a 2,3,5-substituted pyridine derivative through a specific ring cleavage reaction. In the synthesis method of the present invention, an enamine structure is formed in situ by using beta keto ester/sulfone/phosphonic acid ester and ammonium acetate and subjected to an aldol condensation reaction with 3-formyl (aza) indole/benzofuran, a cyclization reaction, and a ring-cleavage reaction in that order to synthesize a characteristic pyridine structure having an alkyl/aryl substituent attached to the 2-position thereof, an ester/sulfone/phosphonic acid ester attached to the 3-position thereof, and ortho-aminoaryl/phenol including various substituents attached to the 5-position thereof. In particular, (aza)indole/benzofuran and beta keto ester/sulfone/phosphonic acid ester, which are reaction substrates, are substrates having very high accessibility, and enable the introduction of various substituents, thereby constructing a pyridine skeleton having high biocompatibility into which ortho-aminoaryl or phenol substituents having various substituents are introduced.
专利号:US-2018230111-A1 优先权日:2004-05-21 标 题:Synthesis of tetracyclines and analogues thereof
专利号:US-8598148-B2 优先权日:2004-05-21 标题:Synthesis of tetracyclines and analogues thereof
专利号:US-2010130451-A1 优先权日:2006-04-07 标 题:Synthesis of tetracyclines and analogues thereof
摘要:Spitzner, D., Science of Synthesis, (2005) 15, 68. 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 48. 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 73. 摘要:Spitzner, D., Science of Synthesis, (2005) 15, 69.