- A practical method for the aziridination of α,β-unsaturated carbonyl compounds with a simple carbamate utilizing sodium hypochlorite pentahydrate
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The efficient formation oftert-butylN-chloro-N-sodio-carbamate by the reaction of simpletert-butyl carbamate with sodium hypochlorite pentahydrate (NaOCl·5H2O) would be a practical and green method for the aziridination of α,β-unsaturated carbo
- Minakata, Satoshi,Umeda, Takehiro
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p. 22120 - 22124
(2021/07/02)
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- Stereoselective Synthesis of 1-Aminocyclopropanecarboxylic Acid Carnosadines via Inter-intramolecular Double Alkylation with Optically Active 2-Methylaziridine Derivatives
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The stereoselective and short-step synthesis of N-protected allo-carnosadine, ent-carnosadine, and carnosadine lactam was accomplished from a common cyclopropane intermediate. The inter-intramolecular double alkylation of diethyl malonate with an optically active 2-methylaziridine derivative gave the key cyclopropane in excellent yield and optical purity. The following monohydrolysis of the diester moiety using different reaction conditions provided both diastereomers of monoacids, which were converted to three carnosadine derivatives in 5-6 steps from the common diester.
- Ohsawa, Kosuke,Kubota, Junya,Ochiai, Shota,Doi, Takayuki
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p. 7304 - 7313
(2021/05/29)
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- LZC696 intermediate and synthetic method therefor
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The invention discloses a compound which is (R)-tert-butyl(1,((1,1'biphenyl)-4-yl)3-((t-butyldimethylsilyl)oxo)propane-2-yl)carbamate, and the structural formula of the compound is as shown in formula A in the specification. An LZC696 intermediate is synthetized by adopting the compound, the whole technological process is free of expensive reagents or raw materials, free of sensitive reaction for oxygen and simple in purifying procedure, and commercial using purity can be achieved only by recrystallization purification of the compound 3 and the final product. The synthetic process of the invention is low in cost, simple and environmentally-friendly, and is suitable for industrial mass production.
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Paragraph 0072; 0073
(2016/10/09)
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- Discovery of a new class of glucosylceramide synthase inhibitors
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A novel series of potent inhibitors of glucosylceramide synthase are described. The optimization of biochemical and cellular potency as well as ADME properties led to compound 23c. Broad tissue distribution was obtained following oral administration to mice. Thus 23c could be another useful tool compound for studying the effects of GCS inhibition in vitro and in vivo.
- Koltun, Elena,Richards, Steven,Chan, Vicky,Nachtigall, Jason,Du, Hongwang,Noson, Kevin,Galan, Adam,Aay, Naing,Hanel, Art,Harrison, Amanda,Zhang, Jeff,Won, Kwang-Ai,Tam, Danny,Qian, Fawn,Wang, Tao,Finn, Patricia,Ogilvie, Kathleen,Rosen, Jon,Mohan, Raju,Larson, Christopher,Lamb, Peter,Nuss, John,Kearney, Patrick
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scheme or table
p. 6773 - 6777
(2011/12/05)
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- GLUCOSYLCERAMIDE SYNTHASE INHIBITORS
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The present invention comprises glucosylceramide synthase (GCS) inhibitors of structural formula (I), and pharmaceutically acceptable salts thereof, wherein R1, E, A, L, X1, Q, R4, R5, m and n, are as defined he
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Page/Page column 68
(2010/08/18)
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