1261852-14-5Relevant articles and documents
Pd(II)-Catalyzed Synthesis of Benzocyclobutenes by β-Methylene-Selective C(sp3)-H Arylation with a Transient Directing Group
Chen, Xiangyang,Hoskin, John F.,Houk, K. N.,Provencher, Philip A.,Sorensen, Erik J.,Wong, Jonathan J.,Yu, Jin-Quan
, p. 20035 - 20041 (2021/12/09)
Methylene-selective C-H functionalization is a significant hurdle that remains to be addressed in the field of Pd(II) catalysis. We report a Pd(II)-catalyzed synthesis of benzocyclobutenes by methylene-selective C(sp3)-H arylation of ketones. The reaction utilizes glycine as a transient directing group and a 2-pyridone ligand, which may govern the methylene selectivity by making intimate molecular associations with the substrate during concerted metalation-deprotonation. This reaction is shown to be highly selective for intramolecular methylene C(sp3)-H arylation, thus enabling sequential C(sp3)-H functionalization.
CuSO4-Catalyzed dual annulation to synthesize O, S or N-containing tetracyclic heteroacenes
Kang, Yan-Biao,Qu, Jian-Ping,Shan, Xiang-Huan,Yang, Bo
, p. 4063 - 4066 (2020/04/20)
In this work, CuSO4 is utilized as a practical redox catalyst for tandem dual annulation in the synthesis of indole-fused tetracyclic heteroacenes, which are important skeletons in both medicinal chemistry and materials chemistry. The preparation of such skeletons in a convenient and efficient manner is in high demand. This method realizes the modular synthesis of benzofuro-, benzothieno-, and indoloindoles from abundant feedstocks such as 2-halobenzyl halides and nitrile derivatives in up to 99% yields, providing a rapid access to diverse indole-fused heteroacenes with biological or optoelectronic properties.
A concise synthesis of chiral indanes as α1A adrenoceptor partial agonists
Roberts, Lee R.,Corbett, Matthew S.,Fussell, Steven J.,Hitzel, Laure,Jessiman, Alan S.,Mason, Helen J.,Osborne, Rachel,Ralph, Michael J.,Stennett, Adam S.D.,Wheeler, Simon,Storer, R. Ian
supporting information, p. 6546 - 6550 (2015/11/09)
The synthesis of a series of chiral indanes with reported α1A partial agonist activity is outlined, applying a rhodium catalysed cyclisation for template construction. This method was extended to the asymmetric synthesis of lead compound PF-037