1314079-44-1Relevant articles and documents
Syntheses of Cyclopropyl Analogues of Disorazoles A1 and B1 and Their Thiazole Counterparts
Nicolaou,Buchman, Marek,Bellavance, Gabriel,Krieger, Johannes,Subramanian, Parthasarathi,Pulukuri, Kiran Kumar
, p. 12374 - 12389 (2018)
Modular syntheses of disorazoles A1 and B1 analogues in which the epoxide moieties of the natural products were replaced with cyclopropyl units have been achieved. Targeted as part of a structure-activity relationships study, these syntheses were successfully extended to the thiazole counterparts of these analogues. The retrosynthetically defined fragments were assembled through Yamaguchi esterification, Cu/Pd-catalyzed cross-coupling, Yamaguchi macrolactonization, and Cu-catalyzed cross-coupling as the key reactions. Further synthetic and biological investigations of such analogues are expected to lead to the discovery and development of potential payloads for antibody-drug conjugates as targeted cancer therapies.
Total synthesis of (-)-CP2-disorazole C1
Hopkins, Chad D.,Schmitz, John C.,Chu, Edward,Wipf, Peter
supporting information; experimental part, p. 4088 - 4091 (2011/10/08)
The total synthesis of a bis-cyclopropane analog of the antimitotic natural product (-)-disorazole C1 was accomplished in 23 steps and 1.1% overall yield. A vinyl cyclopropane cross-metathesis reaction generated a key (E)-alkene segment of the