专利号:US-4514569-A 优先权日:1982-01-28 标 题 :Synthesis of 1-substituted isoquinolines 发明人:HENDRICKSON JAMES B; RODRIGUEZ CESAR 权利人:HENDRICKSON JAMES B; RODRIGUEZ CESAR 摘要:A method for the synthesis of particular isoquinoline compounds which are useful intermediates in the preparation of members of the family of opium alkaloids, such as morphine and codeine. Steps in the process include the acylation of the isoquinoline nitrogen; reaction of the acylated isoquinoline with a phosphorous compound; and condensation with a benzaldehyde derivative to yield a 1-benzyl isoquinoline.
专利号:US-5656634-A 优先权日:1991-03-21 标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 发明人:CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:US-5565472-A 优先权日:1992-12-21 标题 :4-aryl-3-(heteroarylureido)-1,2-dihydro-2-oxo-quinoline derivatives as antihypercholesterolemic and antiatherosclerotic agents 发明人:HAMANAKA ERNEST S 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof wherein R 2 , R 3 , R 4 , m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:EP-0623112-B1 优先权日:1992-01-23 标 题:4-Phenyl-3-(heteroarylureido)-1,2-dihydro-2-oxoquinoline derivatives as antihypercholesterolemic and antiatherosclerotic agents 发明人:HAMANAKA ERNEST S 权利人:PFIZER 摘要:Compounds of formula (I) wherein each m is independently selected from 0 to 4; R<2> is selected from hydrogen and (C1-C6) alkyl; each R<3> and R<4> is independently selected from halogen, (C1-C6) alkyl optionally substituted with one or more halogen atoms, (C1-C6) alkoxy optionally substituted with one or more halogen atoms, (C1-C6) alkylthio optionally substituted with one or more halogen atoms; nitro, carboxyl optionally esterified with a (C1-C6) alkyl group; hydroxyl, (C1-C4) acyloxy and (C1-C3) acyl; X is sulfur or oxygen; and Q is a group of formula (XIV), (XV) or (XVI) wherein m is as defined above; n is 0 or 1. Each 1 is independently selected from 0 to 3; each R<6> and R<7> is defined in the description; B, D, E and G are selected from the group consisting of nitrogen and carbon, with the proviso that one or more of B, D and E is nitrogen, and with the proviso that when G is nitrogen, the group XVI is attached to the nitrogen of formula (I) at the 4 or 5 position of the pyrimidine ring (designated by a and b) wherein any of said nitrogens may be oxidized, or the pharmaceutically acceptable salts thereof, and intermediates having formula (IV) used in the synthesis of such compounds. The compounds of formula (I) are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:US-5596001-A 优先权日:1993-10-25 标题 :4-aryl-3-(heteroarylureido)quinoline derivatves 发明人:HAMANAKA ERNEST S 权利人:PFIZER 摘要:Compounds of the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein R 1 , R 2 , R 3 , R 4 , m, X and Q are as defined below, and novel intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and natiatherosclerosis agents.
专利号:CN-115433125-A 优先权日:2022-09-15 标题 :A new method for the synthesis of 2-tert-butoxyquinoline derivatives
摘要:Álvarez, M.; Joule, J. A., Science of Synthesis, (2005) 15, 709. 摘要:Álvarez, M.; Joule, J. A., Science of Synthesis, (2005) 15, 712. 摘要:Ziegler, T., Science of Synthesis, (2005) 21, 68.