专利号:US-12180182-B2 优先权日:2021-12-01 标题 :(Di)amination of activated allene compounds, derivatives thereof, and methods for synthesis of the same 发明人:DAI MINGJI 权利人:PURDUE RESEARCH FOUNDATION 摘要:One-pot synthesis methods for producing amines from activated allenes and derivatives thereof are provided, as well as the compounds produced thereby.
专利号:US-6423871-B1 优先权日:1999-02-26 标题 :Efficient synthesis of secondary amines by selective alkylation of primary amines 发明人:JUNG KYUNG WOON 权利人:UNIV SOUTH FLORIDA 摘要:A method for selective mono-N-alkylation of primary amines to produce secondary amines that are substantially free of overalkylated tertiary amines and quaternary ammonium salts, under mild reaction conditions without the necessity of protecting groups. Compounds of the class of secondary amines are produced by reacting an alkyl halide with an alkyl amine in anhydrous solvent, preferably dimethyl sulfoxide or N,N-dimethylformamide, in the presence of 0.1 to 3 molar equivalents of a cesium base. Optionally, the extent and selectivity of mono-N-alkylation is enhanced by addition to the reaction mixture of a powdered molecular sieve material for removal of water produced by the reaction, and/or tetrabutylammonium iodide to promote halide exchange. The invention permits selective and efficient mono-N-alkylation of a wide variety of substrates at 23° C.; does not cause racemization when used with enantiomerically-pure chiral substrates such as L-α-aminoesters; and is applied to solid phase synthesis whereby either the alkyl amine or alkyl halide is immobilized. The method is additionally used to produce polyamines, such as N-(2-(2-aminoethylthio)ethyl)ethylenediamine in 73% yield.
专利号:US-2023037284-A9 优先权日:2018-11-30 标题:Combination therapy of peptidomimetic macrocycles 发明人:GUERLAVAIS VINCENT; ANNIS DAVID ALLEN 权利人:AILERON THERAPEUTICS INC 摘要:The present disclosure describes the synthesis of peptidomimetic macrocycles and methods of using peptidomimetic macrocycles to treat a condition. The present disclosure also describes methods of using peptidomimetic macrocycles in combination with at least one additional pharmaceutically-active agent for the treatment of a condition, for example, cancer.
专利号:EP-0038869-A1 优先权日:1980-04-30 标 题:Process for the preparation of 1-carbapenems, and intermediates for their preparation 发明人:CHRISTENSEN BURTON G; RATCLIFFE RONALD W 权利人:MERCK & CO INC 摘要:Processes and intermediates for the total synthesis of 1-carbapenem antibiotics (I) via intermediates (III) and (IV):n n wherein R is hydrogen, a pharmaceutically acceptable ester moiety or salt cation, or a readily removable blocking group; R 6 , R 7 and R 8 are, inter alia, independently selected from the group consisting of hydrogen, alkyl, alkenyl, aryl and aralkyl, and X is a conventional leaving group.
专利号:WO-2009117985-A1 优先权日:2008-06-12 标题 :Pirinixic acid derivatives as prostglandin e2 synthesis inhibitors for treating inflammatory diseases 发明人:WERZ OLIVER; KOEBERLE ANDREAS; SCHUBERT-ZSILAVECZ MANFRED; POPESCU LAURA; SYHA YVONNE 权利人:MEDEON PHARMACEUTICALS GMBH; UNIV TUEBINGEN; WERZ OLIVER; KOEBERLE ANDREAS; SCHUBERT-ZSILAVECZ MANFRED; POPESCU LAURA; SYHA YVONNE 摘要:The invention relates to pirinixic acid derivatives, especially a-substituted pirinixic acids and pirinixic acid esters, and the structural derivatives thereof with the following structural formula. The pirinixic acid derivatives inhibit the PGE2 synthesis, especially that of the mPGES-1. The invention also relates to the use of said pirinixic acid derivatives for producing a medicament for treating prostaglandin E2-mediated diseases, especially inflammatory diseases, painful and feverish conditions, cardiovascular events and cancerous diseases associated with an increased inducible microsomal prostaglandin E2 synthesis-1 (mPGES-1) activity or increased prostaglandin E2 synthesis.
专利号:WO-2025217318-A1 优先权日:2024-04-09 标题:Kinetic controlled synthesis for 2d perovskite materials 发明人:MOHITE ADITYA; HOU JIN; AGRAWAL AYUSH 权利人:WILLIAM MARSH RICE UNIV 摘要:Methods of making a two-dimensional perovskite, a two-dimensional perovskite composition are disclosed. The two-dimensional perovskite comprises: a layered material having the formula (I) (A')(A)n-1MnX3n+1, where A' is an organic cation selected from the group consisting of butyl ammonium, 3-(aminomethyl)piperidium (3-AMP), 4- (aminomethyl)piperidium, and combinations thereof; A is a perovskitizer-cation selected from the group consisting of formamidinium (FA), guanidinium, dimethylamine, cesium, and combinations thereof; M is a divalent metal selected from the group consisting of Pb, Ge, Sn, Cu, and combinations thereof; X is a halide selected from the group consisting of I, Br, Cl, F, and combinations thereof; and n is greater than or equal to 2. The layered material comprises alternating layers of a first type and a second type, where the first type comprises the organic cation (A') and the second type comprises a hybrid anion having the formula (II) (A)n-1MnX3n+1, and the layered material has a tetragonal crystal structure with space group symmetry P4/mmm.