专利号:US-4713479-A 优先权日:1986-11-28 标题 :Synthesis of high-purity dialkyl 2-vinylcyclopropane-1,1-dicarboxylate 发明人:CLARK JR CLARENCE E; FAYTER JR RICHARD G 权利人:NAT DISTILLERS CHEM CORP 摘要:This invention relates to a two-step synthesis of high purity dialkyl 2-vinyl-cyclopropane-1,1-dicarboxylate in which a mixture of trans- and cis-1,4-dihalobutene-2 is first isomerized to essentially trans-1,4-dihalobutene-2 followed immediately by cyclocondensing the resultant trans-1,4-dihalobutene-2 with a malonic ester in the presence of an alcoholic solution of a metallic alkoxide.
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-8951728-B2 优先权日:2004-11-22 标 题:Template directed split and mix synthesis of small molecule libraries 发明人:RASMUSSEN PETER BIRK 权利人:CHEMGENE HOLDING APS 摘要:The invention combines the advantages of split and mix synthesis with the advantages of template directed synthesis. The method comprises the steps of: a) adding a linker molecule L to one or more reaction wells; b) adding a molecule fragment to each of said reaction wells; c) adding an oligonucleotide identifier to each of said reaction wells; d) subjecting said wells to conditions sufficient to allow said molecule fragments and said oligonucleotide identifiers to become attached to said linker molecule, or conditions sufficient for said molecule fragments to bind to other molecule fragments and sufficient for said oligonucleotide identifiers to bind to other oligonucleotide identifiers; e) combining the contents of said one or more reaction wells; and f) contacting the resulting bifunctional molecule(s) of step e) with one or more (oligonucleotide) templates each capable of hybridizing to at least one of the oligonucleotide identifiers added in step c).
专利号:US-6297410-B1 优先权日:1997-07-31 标题:Process for the preparation of cyclopropylacetylene 发明人:FORTUNAK JOSEPH M; WANG ZHE; YIN JIANGUO 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor. In the process, cyclopropane carboxaldehyde is condensed with malonic acid to form 3-cyclopropylacrylic acid; 3-cyclopropylacrylic acid is halogenated to form (E,Z)-1-halo-2-cyclopropylethylene; and (E,Z)-1-halo-2-cyclopropylethylene is dehydrohalogenated to form cyclopropyl acetylene. This improvement provides for high conversion of inexpensive, readily available starting materials into cyclopropylacetylene, high overall yields and can be conducted on an industrial scale.
专利号:US-6235957-B1 优先权日:1998-06-29 标 题 :Process for the preparation of cyclopropylacetylene 发明人:CHOUDHURY ANUSUYA 权利人:DU PONT PHARM CO 摘要:The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is an essential reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one; a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.
专利号:US-7232842-B2 优先权日:2003-01-10 标题:Kinase inhibitors and associated pharmaceutical compositions and methods of use 发明人:WENDER PAUL A; SCANIO MARC J 权利人:UNIV LELAND STANFORD JUNIOR 摘要:The invention provides novel compounds useful as kinase inhibitors or as starting materials And/or intermediates in the synthesis of compounds useful as kinase inhibitors. The compounds have The general structure of formula (I) n nwherein A is a 3- to 8-membered ring, optionally substituted and/or heteroatom-containing, and R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , X, Y, Z, p, and q are as defined herein. The compounds may also be in the form of a salt, ester, amide, or other analog. In preferred compounds, A is a 5- to 8-membered ring, R 1 is hydrogen, q is a bond, X is N, Y is Câ•?O, Z is N, R 2 contains a terminal amino moiety, p is 1, and R 3 and R 4 are linked to form a pyrrole ring fused to a second cyclic group. Pharmaceutical compositions and methods for using the compounds are also provided.
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