160886-95-3Relevant academic research and scientific papers
A domino Kornblum-DeLaMare/aza-Michael reaction of 3,6-dihydro-1,2-dioxines and application to the synthesis of the ceramide transport inhibitor (±)-HPA-12
Legendre, Sarah V.A.-M.,Jevric, Martyn,Klepp, Julian,Sumby, Christopher J.,Greatrex, Ben W.
, p. 1229 - 1239 (2017/12/04)
A Kornblum-DeLaMare/aza-Michael reaction of 3,6-dihydro-1,2-dioxines with primary and secondary amines has been developed which affords 4-hydroxy-3-aminoketones. The aza-Michael products were reduced using non-selective NaBH4/MeOH or diastereoselective (up to 92:8) SnCl4/NaBH4 conditions yielding (1R?,3S?)-3-amino-1,4-diols in up to 97% and 70% yield respectively. The major reduction product was converted in two steps to (±)-HPA-12, which is an inhibitor of the cytosolic ceramide transporting protein.
Copper-Catalyzed Addition of Alkylboranes to Iminoacetates: Access to α-Alkyl Branched α-Amino Acids
Xiao, Xinsheng,Zhang, Wei,Lu, Xiaoxia,Deng, Yuanfu,Jiang, Huangfeng,Zeng, Wei
, p. 2497 - 2509 (2016/08/16)
A copper(I)-catalyzed addition of alkylborane reagents to α-iminoacetates has been developed to assemble both acyclic and cyclic α-branched α-amino carboxylic acid derivatives in good yields. A wide variety of unactivated alkenes are well tolerated in this transformation. (Figure presented.).
FUSED THIAZOLE DERIVATIVES AS KINASE INHIBITORS
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Page/Page column 50, (2008/06/13)
A series of 5,6-dihydro-l,3-benzothiazol-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PD kinase enzymes, are accordingly of b.enefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.
Method of treating a neurodegenerative disease by administering an aryl-cyclohexylamine derivative
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, (2008/06/13)
The present invention provides a method of treatment of a disease associated with neurodegeneration by administering a therapeutically effective amount of a compound of the general formula whereinAr1 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by hydroxy, lower alkoxy, nitro, amino or methanesulfonamide;Ar2 is phenyl, naphthyl or tetrahydronaphthyl, optionally substituted by lower alkyl or halogen;X is C, CH, C(OH) or N;Y is —CH2?, CH or O;Z —CH2—, —CH(CH3)— or —C(CH3)2—;R1 is hydrogen, lower alkyl or acetyl;A is C=O or —(CHR2)n—, wherein R2 is hydrogen, lower alkyl or hydroxy-lower alkyl;B is —(CH2)n—, O, —CH(OH)(CH2)n—, —CH(CH2OH)(CH2)n—, —(CH2)n CH(OH)— or —CH(CH2OH)—;- - - may be a bond; andn is 0-4,or pharmaceutically acceptable acid addition salts thereof.
