专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-5861532-A 优先权日:1997-03-04 标 题:Solid-phase synthesis of N-alkyl amides 发明人:BROWN EDWARD G; NUSS JOHN M 权利人:CHIRON CORP 摘要:Methods for solid phase synthesis of N-alkyl amides comprise reductive amination of carbonyl compounds using a reducing agent and an amine-containing linker bound to a solid support. The methods afford high yields of linker-bound, monoalkylated amines, and subsequent coupling with acid derivatives provide derivatized N-substituted amides in excellent yields after cleavage from the solid-phase. Compositions useful in solid phase synthesis are also described.
专利号:US-7470370-B2 优先权日:2003-06-05 标 题 :Process for removal of impurities from mother liquor in the synthesis of carboxylic acid using pressure filtration 发明人:PARKER KENNY RANDOLPH; LIN ROBERT 权利人:EASTMAN CHEM CO 摘要:A process is disclosed that relates to the recovery of a metal catalyst from an oxidizer purge stream produced in the synthesis of carboxylic acid, typically terephthalic. More particularly, the process involves recovery of a metal catalyst from an oxidizer purge stream through the use of a pressure filter, the combining of water with a mother liquor to recover the metal catalyst and then subjecting an aqueous mixture so formed to a single stage extraction with an extraction solvent to produce an extract stream comprising organic impurities and a raffinate stream comprising the metal catalyst.
专利号:US-7494641-B2 优先权日:2003-06-05 标题 :Extraction process for removal of impurities from an oxidizer purge stream in the synthesis of carboxylic acid 发明人:LIN ROBERT; DE VREEDE MARCEL 权利人:EASTMAN CHEM CO 摘要:Disclosed is a process that relates to the recovery of a metal catalyst from an oxidizer purge stream produced in the synthesis of carboxylic acid, typically terephthalic acid. The process involves the addition of a wash solution to a high temperature molten dispersion to recover the metal catalyst and then subjecting an aqueous mixture or purified aqueous mixture so formed to a single stage extraction to remove organic impurities to produce an extract stream and a raffinate stream comprising the metal catalyst.
专利号:US-5889146-A 优先权日:1997-11-26 标题:Method for synthesis of bifunctional chelating agents-peptides 发明人:LEE TE-WEI; CHEN SHUI-TEIN; CHANG SHIANG-RONG; CHYI SHYH-YI; SHING CHANG-MAU; HUANG TIAN-FU; SHEN LIE-HANG; TSAI ZEI-TSAN; WANG KUNG-TSUNG; TING GANN 权利人:INST NUCLEAR ENERGY RES 摘要:This invention is a novel synthesis of BCA-peptides (BCA: bifunctional chelating agents). In this method, the starting material--Fmoc-Thr(ol)-Terephthal-Acetal-Amide Resin is coupled with the various amino acids. The straight peptide-resin of D-Phe-Cys(Trt)-Phe-D-Trp(Boc)-Lys(Boc)-Thr(tBu)-Cys(Trt)-Thr(ol)-Terephthal-Acetal-Amide Resin was obtained. This compound reacted with iodine to give disulfide-containing peptide resin of ##STR1## Cleavage of the peptide from the resin was achieved by TFA. The cleavaged peptide was protected by the reaction of octreotide with di-t-butyldicarbonate. BCA was coupled to the selectively protected octreotide. This product was obtained by reaction of protected BCA-peptides with TFA. The final product was labeled by radioisotope 111 InCl 3 for tumor imaging radiopharmaceuticals.
专利号:US-7452522-B2 优先权日:2003-06-05 标 题 :Extraction process for removal of impurities from an oxidizer purge stream in the synthesis of carboxylic acid 发明人:LIN ROBERT; DE VREEDE MARCEL 权利人:EASTMAN CHEM CO 摘要:Disclosed is a process that relates to the recovery of a metal catalyst from an oxidizer purge stream produced in the synthesis of carboxylic acid, typically terephthalic acid. The process involves the addition of a wash solution to a high temperature molten dispersion to recover the metal catalyst and then subjecting an aqueous mixture or purified aqueous mixture so formed to a single stage extraction to remove organic impurities to produce an extract stream and a raffinate stream comprising the metal catalyst.