427878-69-1Relevant articles and documents
An efficient electrophilic N-amination utilizing in situ generated chloramine under phase transfer conditions
Bhattacharya, Apurba,Patel, Nitin C.,Plata, Robert Erik,Peddicord, Michael,Ye, Qingmei,Parlanti, Luca,Palaniswamy, Venkatapuram A.,Grosso, John A.
, p. 5341 - 5343 (2006)
An efficient, one-pot, phase transfer N-amination technology was developed. The protocol utilizes chloramine, an inexpensive and safe electrophilic aminating agent potentially viable for commercial manufacturing.
TYROSINE KINASE INHIBITOR AND PHARMACEUTICAL COMPOSITION COMPRISING SAME
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Paragraph 0230; 0232, (2018/03/25)
The present invention relates to a tyrosine kinase inhibitor and a pharmaceutical composition comprising same. The tyrosine kinase inhibitor of the present invention has the structures as shown in the following formula (I) or (II):
Development of a practical synthesis of a functionalized pyrrolo[2,1-f][1,2,4]triazine nucleus
Zheng, Bin,Conlon, David A.,Corbett, R. Michael,Chau, Melissa,Hsieh, Dau-Ming,Yeboah, Agnes,Hsieh, Daniel,Mueslehiddinoglu, Jale,Gallagher, William P.,Simon, Jeffrey N.,Burt, Justin
, p. 1846 - 1853 (2013/01/15)
Functionalized pyrrolotriazine 1b is a key heterocyclic building block in the synthesis of BMS-690514, a potent anticancer agent. Described herein are our development activities that led to the efficient preparation of 1b on a large scale. The key transformations include a selective C-alkylation of an oxalacetate salt with a hydrazonyl bromide to form a 2-hydrazonoethyl-3- oxosuccinate, followed by cyclodehydration to an aminopyrrole. Subsequent deprotection and condensation with formamidine afforded the pyrrolotriazine scaffold. Further elaboration of this core provided the desired pyrrolotriazinyl amine.