- A new concise synthesis of (+)-ipomeamarone, (-)-ngaione, and their stereoisomers
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A new concise and enantiocontrolled total synthesis of (+)-ipomeamarone (1), a well-known phytoalexin, is described. The key step involved a tetrahydrofuran ring construction from optically active furyl alcohol 5 via the π-allyl palladium complex with a chiral phosphine ligand. This procedure was also applicable to the synthesis of (1)-ngaione (2) and its stereoisomers.
- Usuki, Yoshinosuke,Deguchi, Taku,Iio, Hideo
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p. 1882 - 1884
(2015/02/05)
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- Retinoid-like heterocycles
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This invention relates to a compound of formula I STR1 in which T is --CONH-- or --CH CH--;R a and R b are independently C 1-6 alkyl;R c is C 1-6 alkyl or hydrogen; andR is heteroaryl and these compounds are useful in preventing and treating skin disorder
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- 14β-H-, 14-and 15-En-11β-aryl-4-oestrenes
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Novel compounds of the general formula I STR1 and the pharmacologically tolerable addition salts thereof with acids are described, in which eitherIa) R 11 represents a hydrogen atom in the β-configuration and each of R 12 and R 13 represents a hydrogen atom, orIb) R 11 represents a hydrogen atom in the β-configuration and R 12 and R 13 together represent a second bond, orIc) R 11 and R 12 together represent a second bond and R 13 represents a hydrogen atom, orId) R 11 represents a hydrogen atom in the α-configuration and R 12 and R 13 together represent a second bond,and in Ia), Ib), Ic) or Id)X represents an oxygen atom, the hydroxyimino grouping >N OH or two hydrogen atoms,R 1 represents a hydrogen atom or a methyl group,R 2 represents a hydroxy group, a C 1 -C 10 -alkoxy group or a C 1 -C 10 -acyloxy group, andR 3 and R 4 have the meanings customary for competitive progesterone antagonists specified in the description.The invention relates also to processes for the preparation of the novel compounds, to pharmaceutical compositions containing those compounds, to their use for the manufacture of medicaments, and to the novel intermediates required for the process.The novel compounds have a strong affinity for the gestagen receptor and exhibit pronounced antigestagenic and also antiglucocorticoid, antimineralocorticoid and antiandrogenic properties.
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- 3,4-Bis(tributylstannyl)furan: a Versatile Building Block for the Regiospecific Synthesis of 3,4-Disubstituted Furans
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By utilising an oxazole-alkyne Diels-Alder reaction, 3,4-bis(tributylstannyl)furan is prepared and its synthetic potential assessed by its conversion into several 3,4-disubstituted furans via Stille-type palladium-catalysed reactions.
- Yang, Yun,Wong, Henry N. C.
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p. 656 - 658
(2007/10/02)
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- THE CHEMISTRY OF ORGANOLEAD(IV) TRICARBOXYLATES. SYNTHESIS AND ELECTROPHILIC HETEROARYLATION REACTIONS OF 2- AND 3-THIENYL-, AND 2- AND 3-FURYL-LEAD
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Tin(IV)-lead(IV) exchange and mercury(II)-lead(IV) exchange reactions have been used to obtain 2-thienyl-lead triacetate (3), 2-thienyl-lead tribenzoate (4), 3-thienyl-lead triacetate (16), 2-furyl-lead triacetate (21), and 3-furyl-lead triacetate (31).In reactions with the β-dicarbonyl compounds (7), (11), and (13), the above heteroaryl-lead compounds behaved as 2-thienyl, 3-thienyl, 2-furyl, and 3-furyl cation equivalents respectively, giving the α-heteroaryl β-dicarbonyl compounds (8), (12), (14), (17), (18), (19), (25), (27), (28), (38), (34), and (35) in synthetically useful yields.
- Pinhey, John T.,Roche, Eric G.
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p. 2415 - 2422
(2007/10/02)
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