- HIV PROTEASE INHIBITORS
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The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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Page/Page column 24; 25
(2015/07/07)
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- Two syntheses of (-)-kainic acid via highly stereoselective zinc-ene cyclizations
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Two concise, high-yielding syntheses of enantioenriched (-)-kainic acid are presented. Both routes feature a Pd-catalyzed Zn-ene cyclization that proceeds with complete diastereoselectivity. The key step can be carried out on a multigram scale, and the ov
- Chalker, Justin M.,Yang, Ao,Deng, Kai,Cohen, Theodore
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p. 3825 - 3828
(2008/02/12)
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- Novel approach to the (-)-sparteine-mediated synthesis of kainoids: Total synthesis of (-)-α-kainic acid by (-)-sparteine-mediated deprotonation
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We report a new synthesis of kainoids via allyllithium compounds using an intramolecular cycloalkylation as the key step. Preparation of different substituted pyrrolidines was carried out by using carbamates, that react with the chiral base n-BuLi/(-)-sparteine with strong selection between the diastereotopic protons adjacent to the carbamate group in favour for the pro-S proton. (-)-α-Kainic acid was synthetized from D-serine methyl ester hydrochloride, based on a (-)-sparteine-mediated asymmetric deprotonation of an intermediate carbamate that, by stereospecific anti-SN′S E′ intramolecular cycloalkylation, leads to the pyrrolidine ring precursor of (-)-α-kainic acid, in high yield and diastereoselectivity. Related approaches, starting from L-glutamic acid failed. The intermediate pyrrolidine was further transformed to (-)-α-kainic in three steps. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2005.
- Martinez, M. Montserrat,Hoppe, Dieter
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p. 1427 - 1443
(2007/10/03)
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- Total synthesis of (-)-α-kainic acid by (-)-sparteine-mediated asymmetric deprotonation-cycloalkylation
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(Chemical Equation Presented) We report a new enantioselective synthesis of (-)-α-kainic acid from D-serine methyl ester hydrochloride, based on a (-)-sparteine-mediated asymmetric deprotonation of an intermediate carbamate that, by stereospecific anti SN′SE′ intramolecular cycloalkylation, leads to the pyrrolidine ring precursor of (-)-α-kainic acid, in high yield and diastereoselectivity. The intermediate pyrrolidine was further transformed to (-)-α-kainic acid in three steps.
- Martinez, M. Montserrat,Hoppe, Dieter
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p. 3743 - 3746
(2007/10/03)
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