专利号:US-9475780-B2 优先权日:2011-07-20 标 题 :Process for the synthesis of cyclic alkylene ureas 发明人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE 权利人:GUPTA RAM; KOBYLANSKA IRINA; TREASURER URVEE; FLOOD LAWRENCE; ALLNEX IP S AR L 摘要:The invention relates to a process for the synthesis of cyclic alkylene ureas comprising reacting in the presence of a basic catalyst, a difunctional amine A having two primary amino groups, and an aliphatic organic carbonate component C selected from the group consisting of dialkyl carbonates CD and of alkylene carbonates CA, wherein the ratio of the amount of substance Ji(—NH2) of primary amino groups —NH2 in the difunctional amine A to the sum M(C) of the amount of substance n(CD) of carbonate groups of a dialkyl carbonate CD and the amount of substance n(CA) of carbonate groups in an alkylene carbonate CA, is at least more than 2, and to the product obtained by this process.
专利号:US-4627968-A 优先权日:1984-09-10 标 题 :Synthesis of crystalline aluminosilicate with alkylurea or alkylthiourea 发明人:KAI TADASHI 权利人:ASAHI CHEMICAL IND 摘要:In the synthesis of a crystalline aluminosilicate by heating an aqueous mixture containing a silica source, an alumina source and an alkali metal source, at least one compound selected from lower alkylureas and lower alkylthioureas is permitted to co-exist with the mixture.
专利号:US-5362899-A 优先权日:1993-09-09 标题:Chiral synthesis of alpha-aminophosponic acids 发明人:CAMPBELL DAVID A 权利人:AFFYMAX TECH NV 摘要:A stereospecific method of preparing alpha-aminophosphonic acids and derivatives thereof is provided. A protected amino acid is converted to a acyl aroyl or diacyl peroxide which spontaneously rearranges to form an alpha-amino ester. This rearrangement occurs stereospecifically with retention of configuration. The ester is subsequently converted to an appropriate leaving group and displaced with a phosphite yielding a chiral alpha-aminophosphonic acid or derivative. n Alpha-aminophosphonic acids are useful for the synthesis of peptide analogs that possess a phosphonate linkage in the place of an amide linkage. This substitution can impart protease resistance in therapeutic peptides thereby increasing the serum half-life.
专利号:US-9221821-B2 优先权日:2012-06-05 标题:Methods for the synthesis of 1,3-substituted aminouracils and other xanthine-related compounds 发明人:DIEP NHUT; KALYAN YURIY B 权利人:FOREST LAB HOLDINGS LTD; FOREST LAB HOLDINGS LTD 摘要:Methods for the synthesis of disubstituted aminouracils and xanthine and/or xanthine-related compounds are provided.
专利号:US-11633492-B2 优先权日:2017-11-24 标题 :Process for the synthesis of linker-drug vc-seco-DUBA 发明人:JANOUSEK VLADIMIR; KAS MARTIN 权利人:BYONDIS BV 摘要:The compound of formula (II) is an advantageous intermediate for improving the process of synthesizing the linker-drug vc-seco-DUBA, as well as for the overall process for preparing an antibody-drug conjugate comprising the vc-seco-DUBA linker-drug. The methods of making the compound of formula (II) can include recovery of the compound as a solid, such as via crystallization, in high yields and purity.
专利号:US-8501941-B2 优先权日:2005-02-25 标题 :Methods for the synthesis of unsymmetrical cycloakyl substituted xanthines 发明人:WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D 权利人:WANG GUOQUAN; RIEGER JAYSON M; THOMPSON ROBERT D; DOGWOOD PHARMACEUTICALS INC 摘要:The present invention provides compounds and pharmaceutical compositions that are selective antagonists of A 2B adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents. Also provided are processes for the preparation of the compounds and their intermediates.
摘要:Journal of Pharmacology and Experimental Therapeutics., 52(216), 1934 摘要:Schafer, E. W., Jr., and W. A. Bowles Jr. 1985. Acute oral toxicity and repellency of 933 chemicals to house and deer mice. Archives of Environmental Contamination and Toxicology 14:111-129. https://www.aphis.usda.gov/ws/nwrc/chem-effects-db/S_schafer851.pdf