- FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Aβ production inhibitory effect or a BACE1 inhibitory effect and is useful as a prophylactic or therapeutic agent for a neurodegenerative disease caused by Aβ and typified by Alzheimer-type dementia.
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Page/Page column
(2014/07/08)
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- Stereoselective synthesis of dienyl phosphonates via extended tethered ring-closing metathesis
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Allylphosphonates of allylic alcohols were converted to conjugated dienyl phosphonates in a one-flask reaction, comprising a ring-closing metathesis (RCM), a base-induced ring-opening, and an alkylation. The ring-opening proceeds with very high diastereoselectivity, giving exclusively the (1Z,3E)-configured dienes. Single diastereomers and mixtures of diastereomers can be used as starting materials without noticeable effect on the diastereoselectivity of the sequence.
- Schmidt, Bernd,Kunz, Oliver
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supporting information
p. 4470 - 4473
(2013/09/24)
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- FUSED AMINODIHYDROTHIAZINE DERIVATIVES
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The present invention relates to a fused aminodihydrothiazine derivative of formula (I): wherein X is hydrogen or fluorine; R is monofluoromethyl or difluoromethyl; and pharmaceutically acceptable salts thereof; which compound has an Αβ production inhibit
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Page/Page column 69-70
(2012/08/07)
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- A modular approach to aryl-C-ribonucleosides via the allylic substitution and ring-closing metathesis sequence. A stereocontrolled synthesis of all four α-/β- and D-/L-C-nucleoside stereoisomers
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Iridium(I)-catalyzed allylation of the enantiopure monoprotected copper(I) alkoxide, generated from (S)-5a, with the enantiopure allylic carbonates (R)-9a,b has been developed as the key step in a new approach to C-nucleoside analogues. The anomeric cente
- Stambasky, Jan,Kapras, Votech,Stefko, Martin,Kysilka, Ondrej,Hocek, Michal,Malkov, Andrei V.,Kocovsky, Pavel
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experimental part
p. 7781 - 7803
(2011/12/14)
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- Synthesis of 3-oxooxa- and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K
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3-Oxooxa- and 3-oxoazacycloalk-4-enes were obtained with good yield from 1-(ω-alkenyloxy)- and 1-(ω-alkenylamino)-but-3-en-2-ones by using a ring-closing metathesis. This methodology has been used to synthesize an inhibitor of cathepsin K.
- Taillier, Catherine,Hameury, Thomas,Bellosta, Véronique,Cossy, Janine
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p. 4472 - 4490
(2008/02/01)
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- Stereoselective synthesis of (E)- and (Z)-3-hydroxy-2-methyl-1-alkenyl iodides by base-promoted ring-opening of iodomethylated epoxides
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Both (E)- and (Z)-3-hydroxy-2-methyl-1-alkenyl iodides were stereoselectively synthesized from iodomethylated epoxides by treatment with sodium hexamethyldisilazane in DMF and with LDA in THF (or lithium 2,2,6,6-tetramethylpiperidide in THF), respectively
- Ichige, Takahiro,Matsuda, Daisuke,Nakata, Masaya
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p. 4843 - 4848
(2007/10/03)
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- Generation of 2-substituted-2-metallo-1,3-dithianes and their coupling with 1,2-disubstituted epoxides at room temperature
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2-Substituted-1,3-dithianes were subjected to lithiation by n-BuLi at room temperature and the resulting anions reacted with 1,2-disubstituted epoxides at room temperature, giving the coupling products in satisfactory yield. In addition, a mixed organomet
- Ide, Mitsuaki,Yasuda, Minora,Nakata, Masaya
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p. 936 - 938
(2007/10/03)
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