124338-52-9Relevant academic research and scientific papers
Asymmetric Induction by a Nitrogen14N/15N Isotopomer in Conjunction with Asymmetric Autocatalysis
Matsumoto, Arimasa,Ozaki, Hanae,Harada, Shunya,Tada, Kyohei,Ayugase, Tomohiro,Ozawa, Hitomi,Kawasaki, Tsuneomi,Soai, Kenso
, p. 15246 - 15249 (2016/12/03)
Chirality arising from isotope substitution, especially with atoms heavier than the hydrogen isotopes, is usually not considered a source of chirality in a chemical reaction. An N2,N2,N3,N3-tetramethyl-2,3-butan
The lab oddity prevails: Discovery of Pan-CDK inhibitor (R)-S-Cyclopropyl-S-(4-{[4-{[(1R,2R)-2-hydroxy-1-methylpropyl]oxy}-5-(trifluoromethyl)pyrimidin-2-yl]amino}phenyl)sulfoximide (BAY1000394) for the treatment of cancer
Luecking, Ulrich,Jautelat, Rolf,Krueger, Martin,Brumby, Thomas,Lienau, Philip,Schaefer, Martina,Briem, Hans,Schulze, Julia,Hillisch, Alexander,Reichel, Andreas,Wengner, Antje Margret,Siemeister, Gerhard
, p. 1067 - 1085 (2013/07/26)
Lead optimization of a high-throughput screening hit led to the rapid identification of aminopyrimidine ZK304709, a multitargeted CDK and VEGF-R inhibitor that displayed a promising preclinical profile. Nevertheless, ZK304709 failed in phaseI studies due
PROCESS FOR PREPARING PAN-CDK INHIBITORS OF THE FORMULA (I), AND INTERMEDIATES IN THE PREPARATION
-
, (2013/09/26)
The invention relates to a novel process for the preparation of pan-CDK inhibitors of the formula (I), and intermediates of the preparation.
SULFONE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS A MEDICINE
-
Page/Page column 6-7, (2011/10/19)
The invention relates to sulphone-substituted anilinopyrimidine derivatives of the formula (I), to its preparation processes, and to its use as medicament for treating various diseases.
SULFOXIMINE-SUBSTITUTED ANILINOPYRIMIDINE DERIVATIVES AS CDK INHIBITORS, THE PRODUCTION THEREOF, AND USE AS MEDICINE
-
Page/Page column 7, (2011/12/13)
The invention relates to sulfoximine-substituted anilino-pyrimidine derivatives of formula (I). methods of production thereof, and use thereof as medication for the treatment of various diseases.
Reductive cleavage of acetals and ketals with 9-borabicyclo[3.3.1]nonane
Soderquist, John A.,Kock, Iveliz,Estrella, Maria E.
supporting information, p. 1076 - 1079 (2012/12/23)
The reductive cleavage of benzaldehyde acetals and acetophenone ketals with the air-stable crystalline 9-borabicyclo[3.3.1]-nonane dimer provides monobenzylated ether derivatives of diols and 1,2-oxygen-transposed β-phenethyl alcohols, respectively. The boron moiety is effectively recovered through simple procedures which involve convenient air-stable reagents and boron byproducts. The process is particularly selective for 1,3-diols giving the more substituted monobenzyl ether derivatives exclusively. With acetophenone ketals both reduction and elimination occur, permitting 9-BBN-H to hydroborate the resulting styrene to produce 1,2-oxygen-transposed β-phenethyl alcohols cleanly. Potential applications of this new process were illustrated with the synthesis of the hallucinogen, mescaline, and the analgesic, ibufenac.
Hydroxylated analogues of the orally active broad spectrum antifungal, Sch 51048 (1), and the discovery of posaconazole [Sch 56592; 2 or (S,S)-5]
Bennett, Frank,Saksena, Anil K.,Lovey, Raymond G.,Liu, Yi-Tsung,Patel, Naginbhai M.,Pinto, Patrick,Pike, Russel,Jao, Edwin,Girijavallabhan, Viyyoor M.,Ganguly, Ashit K.,Loebenberg, David,Wang, Haiyan,Cacciapuoti, Anthony,Moss, Eugene,Menzel, Fred,Hare, Roberta S.,Nomeir, Amin
, p. 186 - 190 (2007/10/03)
As part of a detailed study, the syntheses, biological activities, and pharmacokinetic properties of hydroxylated analogues of the previously described broad spectrum antifungal agents, Sch 51048 (1), Sch 50001 (3), and Sch 50002 (4), are described. Based on an overall superior profile, one of the alcohols, Sch 56592 (2), was selected for clinical studies.
Diastereoselectivity in the reduction of α-oxy- and α-amino-substituted acyclic ketones by polymethylhydrosiloxane
Nadkarni, Durgesh,Hallissey, James,Mojica, Carlos
, p. 594 - 596 (2007/10/03)
Diastereoselectivity in the reduction of α-alkoxy-, α-acyloxy-, and α-alkylamino-substituted ketones with polymethylhydrosiloxane (PMHS) in the presence of fluoride ion catalysis was investigated. High syn-selectivity was observed in the reduction of α-alkoxy, α-acyloxy, and α-dialkylamino ketones. Reduction of α-monoalkylamino ketone proceeded in anti-selective manner with moderate selectivity. The observed selectivity is explained based on Felkin-Anh and Cram-chelate models.
Hydrogenation of α-Keto Ethers: Dynamic Kinetic Resolution with a Heterogeneous Modified Catalyst and a Heterogeneous Base
Studer, Martin,Blaser, Hans-Ulrich,Burkhardt, Stephan
, p. 511 - 515 (2007/10/03)
The first successful example of the asymmetric hydrogenation of substituted α-keto ethers with Cinchona-modified Pt/Al2O3 is reported. In the absence of an additional base, kinetic resolution of the racemic starting material was observed with high diastereoselectivity and ee's up to 98% at conversions of a strong reaction acceleration but racemic product. Immobilization of OH- on solid ion exchangers resulted in the desired dynamic kinetic resolution, and ee's of >80% were obtained at >95% conversion. These effects are rationalized on the basis of a simple kinetic and structural model.
Chelation-controlled reduction of α- and β-oxygenated ketones with lithium tri-n-butylborohydride
Faucher, Anne-Marie,Brochu, Christian,Landry, Serge R.,Duchesne, Isabelle,Hantos, Susanne,Roy, Amelie,Myles, Andrew,Legault, Claude
, p. 8425 - 8428 (2007/10/03)
Lithium tri-n-butyl borohydride showed high selectivity in the reduction of α- and β-oxygenated ketones, giving a preponderance of the chelation controlled products.
