专利号:US-3959322-A 优先权日:1960-09-22 标 题:Synthesis of 13-alkyl-gon-4-ones 发明人:HUGHES GORDON ALAN; SMITH HERCHEL 权利人:SMITH HERCHEL 摘要:The preparation of 13-methylgon-4-enes and novel 13-polycarbonalkylgon-4-enes by a new total synthesis is described. 13-Alkylgon-4-enes having progestational, anabolic and androgenic activities are prepared by forming a tetracylic gonane structure unsaturated in the 1,3,5(10),9(11) and 14-positions, selectively reducing in the B- and C-rings, and converting the aromatic A-ring compounds so-produced to gon-4-enes by Birch reduction and hydrolysis.
专利号:US-5194671-A 优先权日:1991-05-23 标题 :Process for the preparation of β-ketocarboxylic acid esters 发明人:MEIER JOSEF 权利人:WACKER CHEMIE GMBH 摘要:The invention relates to a process for the preparation of β-ketocarboxylic acid esters of the general formula ##STR1## in which R 1 is an alkyl radical having 1 to 4 C atoms, R 2 is an alkyl radical or alkenyl radical having 2 to 15 C atoms or a phenyl radical and R 3 is hydrogen or an alkyl or alkenyl radical having 1 to 6 C atoms, characterized in that acetocarboxylic acid esters of the general formula ##STR2## in which R 1 and R 3 are as defined, are reacted with calcium hydroxide or calcium oxide in the presence of an organic solvent and in the absence of water, the calcium chelate complexes formed are acylated with carboxylic acid chloride and the products are then cleaved with aqueous ammonium salt solution to form the β-ketocarboxylic acid esters of formula (I). n The β-ketocarboxylic acid esters readily accessible by the process according to the invention can be used as important intermediates in the synthesis of pharmaceutically active ingredients or plant protection agents.
专利号:WO-2010115869-A1 优先权日:2009-04-03 标 题 :Propofol phosphonyl derivatives, synthesis, and use in long acting formulations 发明人:GONNISSEN YVES RENE JOHANNA PAUL 权利人:SEPS PHARMA N V; GONNISSEN YVES RENE JOHANNA PAUL 摘要:This invention relates to compounds represented by the structural formula (I), and the salts and stereoisomers thereof, wherein: - L is a linker selected from the group consisting of -(CH 2 ) P -O-, a single bond, formula (IA), -(CH 2 ) 1-8 -O-X(O)-, and - p is an integer from 1 to 8, - each R 3 and each R 4 is independently selected from the group consisting of C 1-20 alkyl, C 3-12 alkyl, C 3-12 cycloalkyl-C 1-4 alkyl, saturated heterocyclyl and saturated heterocyclyl-C 1-4 alkyl, and - X and Y are each independently C or S(O), - Z is selected from the group consisting of O, S(O) and NR 5 , - W is selected from the group consisting of halogen, OH, S(O)H and O - M + wherein M + is a monovalent cation; and - R 5 is selected from the group consisting of hydrogen and C 1-10 alkyl. These compounds are useful pharmaceutical agents with improved oral bioavailability.
专利号:US-3636119-A 优先权日:1969-10-20 标题:4-amino-2-(8-cyclohexyloctyl or 7-cyclohexylheptyl)-1-naphthol 发明人:FIESER LOUIS F; LORENZ ROMAN R; ARCHER SYDNEY 权利人:FIESER LOUIS F; ROMAN R LORENZ; SYDNEY ARCHER 摘要:4-AMINO-2-Q-1 NAPHTHOL COMPOUNDS WHICH ARE USEFUL AS INTERMEDIATES IN THE SYNTHESIS OF 2-Q-1,4-NAPHTHOQUINONE COMPOUNDS, WHERE Q IS (7-CYCLOHEXYLHEPTYL OR 8-CYCLOHEXYLOCTYL).
专利号:US-4160862-A 优先权日:1972-06-12 标 题 :1-Acyl-3-(amino-lower-alkyl)indoles 发明人:ZENITZ BERNARD L 权利人:STERLING DRUG INC 摘要:1-Acyl-3-(amino-lower-alkyl)indoles, useful as anti-inflammatory agents, are prepared either by acylation of a 3-(amino-lower-alkyl)indole; by Fisher indole synthesis from an N'-acylphenylhydrazine and an amino-lower-alkanone; by alkylation of an amine with a 1-acyl-3-(halo-lower-alkyl)indole; or by reductive alkylation of a 1-acyl-3-indole-lower-alkylcarboxaldehyde.
专利号:US-4021431-A 优先权日:1972-06-12 标 题:3-(Piperidino-lower-alkyl)-indoles 发明人:ZENITZ BERNARD L 权利人:STERLING DRUG INC 摘要:1-Acyl-3-(amino-lower-alkyl)indoles, useful as anti-inflammatory agents, are prepared either by acylation of a 3-(amino-lower-alkyl)indole; by Fisher indole synthesis from an N'-acylphenylhydrazine and an amino-lower-alkanone; by alkylation of an amine with a 1-acyl-3-(halo-lower-alkyl)indole; or by reductive alkylation of a 1-acyl-3-indole-lower-alkylcarboxaldehyde.