The invention concerns quinazoline derivatives of the formula I ##STR1## wherein X.sup.1 is a direct link or a group such as CO, C(R.sup.2).sub.2 and CH(OR.sup.2); wherein Q.sup.1 is phenyl, naphthyl or a 5- or 6-membered heteroaryl moiety and Q.sup.1 optionally bears up to 3 substituents; wherein m is 1 or 2 and each R.sup.1 may be a group such as hydrogen, halogeno and trifluoromethyl; and wherein Q.sup.2 may be phenyl or a 9- or 10-membered bicyclic heterocyclic moiety and Q.sup.2 optionally bears up to 3 substituents; or a pharmaceutically-acceptable salt thereof; processes for their preparation, pharmaceutical compositions containing them and the use of their receptor tyrosine kinase inhibitory properties in the treatment of proliferative disease such as cancer.
Enantioselective Multicomponent Condensation Reactions of Phenols, Aldehydes, and Boronates Catalyzed by Chiral Biphenols
作者:Keith S. Barbato、Yi Luan、Daniele Ramella、James S. Panek、Scott E. Schaus
DOI:10.1021/acs.orglett.5b02954
日期:2015.12.4
Chiral diols and biphenolscatalyze the multicomponent condensation reaction of phenols, aldehydes, and alkenyl or aryl boronates. The condensation products are formed in good yields and enantioselectivities. The reaction proceeds via an initial Friedel–Crafts alkylation of the aldehyde and phenol to yield an ortho-quinone methide that undergoes an enantioselectiveboronateaddition. A cyclization
Process for lithium mono- and diorganylborohydrides
申请人:Aldrich-Boranes, Inc.
公开号:US04772751A1
公开(公告)日:1988-09-20
Improved processes for liberating boronic, RB(OR').sub.2, and borinic, RR'BOR', esters from their "ate" complexes, free of alcohol are provided. Pyrolysis of lithium organylborates LiRB(OR').sub.3 and LiRR'BOR', wherein R is an organyl group and R' is straight or branched-chain lower alkyl, directly yields the relatively volatile boronic and borinic esters in high purity, leaving behind a residue of lithium alkoxide. Treatment of the lithium organylborates with an appropriate acid halide cleanly liberates either volatile or non-volatile boronic or borinic esters, readily separated from the lower alkyl ester produced as a by-product. The novel compound lithium dimethylborohydride is also provided.
Chiral synthesis via organoboranes. 10. Preparation of .alpha.-chiral acyclic ketones of exceptionally high enantiomeric excess from optically pure borinic esters
作者:Herbert C. Brown、Morris Srebnik、Raman K. Bakshi、Thomas E. Cole
DOI:10.1021/ja00252a018
日期:1987.9
BROWN, HERBERT C.;SREBNIK, MORRIS;BAKSHI, RAMAN K.;COLE, THOMAS E., J. AMER. CHEM. SOC., 109,(1987) N 18, 5420-5426
作者:BROWN, HERBERT C.、SREBNIK, MORRIS、BAKSHI, RAMAN K.、COLE, THOMAS E.