CAS: 10147-36-1; Propane-1-Sulfonyl Chloride

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专利信息

专利号:US-6639059-B1
优先权日:1999-03-24
标 题 :Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.

专利号:US-6734291-B2
优先权日:1999-03-24
标题:Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs

专利号:US-9604911-B2
优先权日:2013-12-05
标题 :Process for the synthesis of agomelatine
发明人：BRIERE JEAN-FRANÇOIS; LEBEUF RAPHAËL; LEVACHER VINCENT; HARDOUIN CHRISTOPHE; LECOUVE JEAN-PIERRE
权利人:SERVIER LAB
摘要:Process for the industrial synthesis of the compound of formula (I):

专利号:US-9695169-B2
优先权日:2012-05-31
标 题:Synthesis of heterocyclic compounds
发明人：IBRAHIM PRABHA N
权利人:PLEXXIKON INC
摘要:Provided herein are intermediates and processes useful for facile synthesis of biologically active molecules.

专利号:US-6288297-B1
优先权日:1998-10-01
标 题:Process for the preparation of cyclopropylacetylene
发明人：WANG ZHE; YIN JIANGUO; FORTUNAK JOSEPH M; CAMPAGNA SILVIO
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, for example, cyclopropane carboxaldehyde is alkylated to form 1,1,1-trichloro-2-cyclopropyl-ethanol; which in turn is hydroxy protected to form 1,1,1-trichloro-2-cyclopropylethyltosylate; which in turn undergoes elimination 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-4683323-A
优先权日:1984-07-31
标 题:Method for inversion of optically active 4-hydroxy-2-cyclopentenones
发明人：MINAI MASAYOSHI; UEDA YUJI
权利人:SUMITOMO CHEMICAL CO
摘要:By hydrolyzing a sulfonic acid ester or a nitric acid ester of an optically active 4-hydroxy-2-cyclopentenone, the steric inversion of the hydroxyl group at the 4-position of the cyclopentenone mentioned above is effected. n 4-hydroxy-2-cyclopentenone is useful as a raw material of prostaglandins (natural substance is an (R)-substance) having stimulative action to uterine muscle and vasodilator action. For instance, 4(S)-hydroxy-2-cyclopentenone can be configurationally inverted to R-isomer. Accordingly, this method is extremely meaningful in the synthesis of prostaglandins.