专利号:WO-2025136243-A1 优先权日:2023-12-20 标题:Mechanochemical synthesis of histamine h1-receptor antagonists 发明人:AYDONAT SIMAY; OZEL MERTCAN; YIGITBASI JOANNA MARIANNA; BAYTEKIN BILGE; COLACINO EVELINA 权利人:IHSAN DOGRAMACI BILKENT UNIV; CENTRE NAT RECH SCIENT 摘要:The present invention relates to mechanochemical synthesis of histamine antagonists which are benzhydryl ethers and unsymmetrically disubstitutes piperazines and salts thereof. Said antihistamine active pharmaceutical ingredients can be diphenhydramine hydrochloride, cyclizine hydrochloride and diphenylpyraline hydrochloride. These antihistamines are used in the treatment of allergies, hives, hay fever (allergic rhinitis), conjunctivitis, reactions to insect bites and sings, nausea, motion sickness, insomnia.
专利号:US-7576234-B2 优先权日:2002-05-15 标题 :Synthesis of 2-alkyl amino acids 发明人:CHORGHADE MUKUND S; GURJAR MUKUND K; MOHAPATRA DEBENDRA K 权利人:GENZYME CORP 摘要:Non-natural amino acids such as 2-alkylated amino acids allow for the synthesis of a wider variety of peptidal and non-peptidal pharmaceutically active agents. A method of preparing a 2-alkyl amino acid involves a Michael-type addition of a nucleophile to a dialkyl 2-methylidenylpropan-1,3-dioate and the conversion of a ester moiety into an amino moiety. The present invention also discloses a method of preparing a class of iron chelating agents related to desferrithiocin, all of which contain a thiazoline ring. In this method, an aryl nitrile or imidate is condensed with cysteine, a 2-alkyl cysteine, or a cysteine ester.
专利号:US-4937334-A 优先权日:1988-07-26 标题:Process for the preparation of intermediates for the synthesis of diltiazem 发明人:CAVICCHIOLI SILVIA; PAIOCCHI MAURIZIO; GIORDANO CLAUDIO 权利人:ZAMBON SPA 摘要:A process for the preparation of the compound (2S,3S)(+)-3-hydroxy-2,3-dihydro-2-(4-methoxyphenyl)-5-(2-dimethylaminoethyl)-1, 5-benzothiazepin-4(5H)-one is described. Said compound is an intermediate useful in the synthesis of Diltiazem.
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-5527824-A 优先权日:1985-07-22 标题 :Substituted Di-T-Butlyphenols useful for inhibiting leukotriene synthesis 发明人:SCHERRER ROBERT A 权利人:RIKER LABORATORIES INC 摘要:Substituted Di-T-Butylphenols useful for inhibiting the synthesis of leukotrienes are disclosed.
专利号:US-7906682-B2 优先权日:2000-08-31 标题 :Synthesis of soluble functionalized lithium initiators 发明人:HALASA ADEL FARHAN; HSU WEN-LIANG 权利人:GOODYEAR TIRE & RUBBER 摘要:This invention discloses a process for making dilithium initiators in high purity. This process can be conducted in the absence of amines which is desirable since amines can act as modifiers for anionic polymerizations. The dilithium compounds made are highly desirable because they are soluble in aromatic solvents. The present invention also discloses a tire which is comprised of a generally toroidal-shaped carcass with an outer circumferential tread, two spaced beads, at least one ply extending from bead to bead and sidewalls extending radially from and connecting said tread to said beads, wherein said tread is adapted to be ground-contacting, and wherein said tread is a cured the rubber formulation which is comprised of (a) at least one rubbery polymer containing functional groups of the structural formula: n nwherein R, R′ and R″ can be the same or different, wherein R is selected from the group consisting of hydrogen atoms, alkyl groups, aryl groups, alkaryl groups, and amino aryl groups, and wherein R′ and R″ represent alkyl groups alkyl groups that contain from 1 to 8 carbon atoms, and (b) at least one member selected from the group consisting of carbon black and silica.