2-溴苯酚置于ruthenium Trichloride,Sodium Periodate,碳酸氢钠,Potassium Carbonate,Cesium Fluoride,N,N-二乙基苯胺体系中,用 甲醇,水,N,N-二甲基甲酰胺 用作溶剂,化学反应 13.91H,反应生成3-溴柳醛 参考文献:A Convenient Preparation Of Salicylaldehydes From 2-Methylbenzofurans By Ozonolysis. 标题:A Convenient Preparation Of Salicylaldehydes From 2-Methylbenzofurans By Ozonolysis. 摘要:将2-甲基苯并呋喃(b)转化为水杨醛(c)的方法是通过在-78oc下用ch2Cl2进行臭氧化反应,随后进行碱性水解,操作方便且有效. Doi:10.1248/cpb.41.1166
专利号:US-9518014-B2 优先权日:2012-07-20 标 题:Process for synthesis of ezetimibe and intermediates used in said process 发明人:DING KUILING; WANG XIAOMING; WANG ZHENG 权利人:SHANGHAI INST ORGANIC CHEMISTRY CAS 摘要:A process for the production of ezetimibe and intermediates used in said process are disclosed. A kind of Morita-Baylis-Hillman adduct can be altered to chiral carboxylic acid derivatives of β-arylamino α-methylene with high activity and selectivity by means of ally lamination reaction, and the above carboxylic acid derivatives of β-arylamino α-methylene can be altered to the chiral intermediates of ezetimibe by means of simple conversion and further synthesized into the chiral drug ezetimibe. The synthesis route introduces chirality through the use of a chiral catalysis method, thereby avoiding the use of the chiral auxiliary oxazolidinone; and the route is economical and eco-friendly.
专利号:US-2024336559-A1 优先权日:2021-10-06 标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids 发明人:OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA 权利人:UNIV NEW YORK STATE RES FOUND 摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.
专利号:US-2022356182-A1 优先权日:2009-03-27 标题 :Inhibitors of hepatitis c virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOLL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-11053243-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; LUDMERER STEVEN W; LIU KUN; WU HAO; SOIL RICHARD; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-9090661-B2 优先权日:2009-03-27 标 题:Inhibitors of hepatitis C virus replication 发明人:COBURN CRAIG A; MCCAULEY JOHN A; LUDMERER STEVEN W; LIU KUN; VACCA JOSEPH P; WU HAO; HU BIN; SOLL RICHARD; SUN FEI; WANG XINGHAI; YAN MAN; ZHANG CHENGREN; ZHENG MINGWEI; ZHONG BIN; ZHU JIAN 权利人:MERCK SHARP & DOHME 摘要:The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.
专利号:US-3957760-A 优先权日:1970-12-16 标 题:Amino acid derivatives 发明人:BODANSZKY MIKLOS 权利人:SQUIBB & SONS INC 摘要:New lactone intermediates useful in the synthesis of peptides are prepared by reacting an α-amino acid with an active carbonyl compound which forms a Schiff's base. The latter is treated with a condensing agent so that cyclization occurs and a lactone is formed from which a peptide may be produced by reaction with an amino acid ester and removal of the protecting groups.