31199-03-8Relevant articles and documents
Catalytic asymmetric hydrogenation of pyrimidines
Kuwano, Ryoichi,Hashiguchi, Yuta,Ikeda, Ryuhei,Ishizuka, Kentaro
supporting information, p. 2393 - 2396 (2015/03/04)
The asymmetric hydrogenation of pyrimidines proceeded with high enantioselectivity (up to 99% ee) using an iridium catalyst composed of [IrCl(cod)]2, a ferrocene-containing chiral diphosphine ligand (Josiphos), iodine, and Yb(OTf)3 (cod=1,5-cyclooctadiene). The chiral catalyst converted various 4-substituted pyrimidines into chiral 1,4,5,6-tetrahydropyrimidines in high yield. The lanthanide triflate is crucial for achieving the high enantioselectivity as well as for activating the heteroarene substrate.
PYRIMIDIN-2-ONE COMPOUNDS AND THEIR USE AS DOPAMINE D3 RECEPTOR LIGANDS
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Page 99; 100, (2010/02/08)
The invention relates to pyrimidin-2-one compounds of general formula (I), in addition to the derivatives and tautomers of (I) and the physiologically acceptable salts of said compounds. In said formula: A represents linear or branched C3-C6 alkene, which can have a double bond or triple bond and/or a group Z, which is not adjacent to the nitrogen atom of the pyrimidinone ring and is selected from O, S, C(O), NR3, C(O)NR3, NR3C(O), OC(O) and C(O)O; B represents a group of formula (II), in which X stands for CH2 or N and Y stands for CH2 or CH2CH2, or X-Y can also jointly represent C=CH, C=CH-CH2 or CH-CH=CH; R1 and R 2 are defined as cited in the description and the claims; and Ar represents an optionally substituted aromatic group. The invention also relates to a pharmaceutical agent, containing at least one compound (I) and the tautomers, derivatives and/or acid addition salts of said compound, optionally together with physiologically acceptable carriers and/or auxiliary agents. The invention also relates to the use of compounds of formula (I), and their tautomers, derivatives and pharmacologically acceptable acid addition salts for producing a pharmaceutical agent for treating diseases, which respond to the influence of dopamine D3 receptor ligands.
Stereospecific synthesis of cryptophycin 1
Li, Lian-Hai,Tius, Marcus A.
, p. 1637 - 1640 (2007/10/03)
Matrix presented A brief stereospecific synthesis of cryptophycin 1 is described in which (R)-mandelic acid serves as the sole source of asymmetry for unit A. The key step is a hetero-Diels-Alder cycloaddition.