2,4,6-三乙基环硼氧烷置于水体系中,化学反应生成 乙基硼酸 参考文献:Organoboron Compounds. Ii. Preparation And Properties Of Some Trialkylboroxines1-3 标题:Organoboron Compounds. Ii. Preparation And Properties Of Some Trialkylboroxines1-3 摘要: DOI:10.1021/ja01576A026
专利号:US-2006287520-A1 优先权日:2005-05-16 标 题 :Synthesis of salinosporamide A and analogues thereof 发明人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 权利人:DANISHEFSKY SAMUEL J; ENDO ATSUSHI 摘要:A novel synthesis of salinosporamide A is provided. Salinospoamide A as well as structurally related natural products, omuralide and lactacystin, have been shown to be proteasome inhibitors. Therefore, these compounds as well as analogues of these natural products may be useful in the treatment of proliferative diseases such as cancer, autoimmune diseases, diabetic retinopathy, etc. The invention provides for the synthesis of salinosporamide A as well as analogs thereof using a convenient point for derivatization of the bicyclic core. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-7910623-B2 优先权日:2005-07-22 标 题 :Synthesis of scabronines and analogues thereof 发明人:DANISHEFSKY SAMUEL J; WATERS STEPHEN P 权利人:SLOAN KETTERING INST CANCER 摘要:A novel synthesis of scabronines, which are related to a broader class of angularly fused tricyclic diterpenoids known as cyathanes, is provided. Scabronine G, its methyl ester derivative, and other analogs have been shown to have neurotrophic activity. Therefore, these compounds are particularly useful in treating neurodegenerative diseases such as Alzheimer's disease, Parkinson's disease, Huntington's diseases, etc. The invention provides for the synthesis of scabronines as well as analogs thereof. Pharmaceutical compositions and method of using the inventive compounds are also provided.
专利号:US-2009221568-A1 优先权日:2005-11-04 标题:Synthesis of Inhibitors of FtsZ 发明人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY 权利人:SHAW JARED; URGAONKAR SAMEER; RAYCHAUDHURI DEBABRATA; LA PIERRE HENRY 摘要:FtsZ, the bacterial analog of tubulin, is a promising new target for developing new antibiotics. It has been shown that polyphenols inhibit the GTPase activity of FtsZ, thereby inhibiting Z-ring formation during mitosis. The present invention provides novel polyphenols compounds, which can be accessed by the synthesis of dichamametin and 2′″-hydroxy-5″-benzylisouvarinol-B as described herein. These novel compounds are useful in treating infections, particularly infections caused by gram-positive organisms. Methods of preparing the inventive compounds are also provided. The compounds are prepared by the benzylation of pinocembrin or chrysin core structure. Pharmaceutical compositions and method of using the compounds to treat disease are also provided. These compounds may be screened for antimicrobial activity as well as other biological activities such as anti-neoplastic, anti-inflammatory, immunosuppressive, and cytotoxic activity.
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-9955664-A1 优先权日:1998-04-24 标 题 :Preparation of carbocyclic compounds 发明人:BECKER MARK W; CHAPMAN HARLAN H; KELLY DAPHNE E; KENT KENNETH M; LEW WILLARD; LOUIE MICHAEL S; MCGEE LAWRENCE R; PRISBE ERNEST J; POSTICH MICHAEL J; ROHLOFF JOHN C; SCHULTZE LISA M; YU RICHARD H; ZHANG LIJUN 权利人:GILEAD SCIENCES INC; BECKER MARK W; CHAPMAN HARLAN H; KELLY DAPHNE E; KENT KENNETH M; LEW WILLARD; LOUIE MICHAEL S; MCGEE LAWRENCE R; PRISBE ERNEST J; POSTICH MICHAEL J; ROHLOFF JOHN C; SCHULTZE LISA M; YU RICHARD H; ZHANG LIJUN 摘要:The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.
专利号:US-6518438-B2 优先权日:1996-08-23 标题:Preparation of cyclohexene carboxylate derivatives 发明人:KENT KENNETH M; KIM CHOUNG U; MCGEE LAWRENCE R; MUNGER JOHN D; PRISBE ERNEST J; POSTICH MICHAEL J; ROHLOFF JOHN C; KELLY DAPHNE E; WILLIAMS MATTHEW A; ZHANG LIJUN 权利人:GILEAD SCIENCES INC 摘要:The present invention provides new synthetic methods and compositions. In particular, new methods of preparing intermediates useful in the synthesis of neuraminidase inhibitors and compositions useful as intermediates that are themselves useful in the synthesis of neuraminidase inhibitors are provided.