73494-49-2Relevant articles and documents
The biogenic amine transporter activity of vinylogous amphetamine analogs
Decker, Ann M.,Partilla, John S.,Baumann, Michael H.,Rothman, Richard B.,Blough, Bruce E.
supporting information, p. 1657 - 1663 (2016/08/24)
A series of vinylogous amphetamine analogs was synthesized and examined for their activity at biogenic amine transporters and serotonin-2 receptor (5-HT2) subtypes. (1S,3E)-1-Methyl-4-phenyl-but-3-enylamine (S-6) is a potent dual dopamine/serotonin (DA/5-HT) releaser with no activity at 5-HT2 receptors. This unique profile of actions suggests that analog S-6 is a viable lead compound for identifying new structural classes of DA/5-HT releasers with therapeutic benefit and reduced abuse liability.
Chemical modification of lipase for rational enhancement of enantioselectivity
Ema, Tadashi,Inoue, Hiroki
supporting information, p. 1374 - 1376 (2015/11/24)
Chemical modifications of the I287C mutant of a Burkholderia cepacia lipase afforded various I287C-X conjugates, among which I287C-PAA bearing an N-phenylacetamide (PAA) moiety showed excellent enantioselectivity and catalytic activity for secondary alcohols. Site-directed chemical modifications are powerful tools to control enantioselective biocatalysis.
Copper(I)-catalyzed boryl substitution of unactivated alkyl halides
Ito, Hajime,Kubota, Koji
, p. 890 - 893 (2012/05/05)
Borylation of alkyl halides with diboron proceeded in the presence of a copper(I)/Xantphos catalyst and a stoichiometric amount of K(O-t-Bu) base. The boryl substitution proceeded with normal and secondary alkyl chlorides, bromides, and iodides, but alkyl sulfonates did not react. Menthyl halides afforded the corresponding borylation product with excellent diastereoselectivity, whereas (R)-2-bromo-5-phenylpentane gave a racemic product. Reaction with cyclopropylmethyl bromide resulted in ring-opening products, suggesting the reaction involves a radical pathway.