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-2022356139-A1 优先权日:2019-09-03 标 题:Synthesis of deuterated aldehydes 发明人:WANG WEI 权利人:ARIZONA BOARD OF REGENTS ON BEHALF OF ATHE UNIV OF ARIZONA 摘要:Described are methods for preparing a deuterated aldehyde using N-heterocyclic carbene catalysts in a solvent comprising D 2 O. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions without functionality manipulation.
专利号:WO-2023112055-A1 优先权日:2021-12-15 标 题 :New synthetic process design for the synthesis of carboxy tormifene and purity analysis to strengthen antidoping testing 发明人:KUMAR GANGASANI JAGADEESH; PAWAR SACHIN DATTRAM; RADHAKRISHNANAND PULLAPANTHULA; MURTY UPADHYAYULA SURYANARAYANA; SAHU PURAN LAL; DUBEY SACHIN; SAHU KAPENDRA; UPADHYAY AWANISH; KUMAR PRAMOD 权利人:DIRECTOR NATIONAL INSTITUTE OF PHARMACEUTICAL EDUCATION AND RES GUWAHATI NIPER G; DIRECTOR NAT DOPE TESTING LABORATORY NDTL 摘要:The present invention relates to a process for preparing a compound of formula I: I. The compound of formula I is useful in anti-doping tests.
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-11512097-B2 优先权日:2019-11-25 标题 :Heterocyclic compounds as Delta-5 desaturase inhibitors and methods of use 发明人:ALLEN JENNIFER R; BELTRANI MICHELA; BOURBEAU MATTHEW P; DAMYANOVA TEODORA P; LINGARD IAIN; MINATTI ANA E; VINCETTI PAOLO 权利人:AMGEN INC 摘要:The present disclosure provides compounds useful for the inhibition of Delta-5 Desaturase (“D5Dâ€?). The compounds have a general Formula I n nwherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, a metabolic or cardiovascular disorder. Further, the disclosure provides intermediates useful in the synthesis of compounds of Formula I.
参考标题:Organocerium Additions To Proline-Derived Hydrazones: Synthesis Of Enantiomerically Enriched Amines 作者:Scott E. Denmark,James P. Edwards,Theodor Weber,David W. Piotrowski |发布日期:2010.5 摘要:The Addition Of Organocerium Reagents (From Both Organolithium And Organomagnesium Precursors) To Chiral Aldehyde Hydrazones Prepared From 1-Aminoproline Derivatives Has Been Studied. The Additions Proceed In Good Yield And High Diastereoselectivity And With Good Nucleophile (Me, N-Bu, I-Pr, T-Bu, Ph, Etc.) And Substrate Scope (Alkyl, Alkenyl And Aryl). The Resulting Hydrazines Can Be Converted To
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摘要:National Technical Information Service., OTS0546424 摘要:Journal of Pharmacology and Experimental Therapeutics., 97(25), 1949