An Efficient Solid-phase Parallel Synthesis of 2-Amino and 2-Amidobenzo(d)oxazole Derivatives via Cyclization Reactions of 2-Hydroxyphenylthiourea Resin
作者： Se-Lin Jung , Seul-Gi Kim , Gee-Hyung Lee , Young-Dae Gong
DOI: 10.5012/BKCS.2012.33.12.4109
关键词:
摘要: An efficient solid-phase methodology has been developed for the synthesis of 2-amino and 2-amidobenzo[d]oxazole derivatives. The key step in this procedure involves preparation polymer-bound 2-aminobenzo[d]oxazole resins 4 by cyclization reaction 2-hydroxyphenylthiourea resin 3. resin-bound 3 is produced addition 2-aminophenol to isothiocyanate-terminated 2 serve as a intermediate linker resin. This core skeleton undergoes functionalization with various electrophiles, such alkylhalides acid chlorides generate 2amino 5 6 respectively. Finally, derivatives 7 8 are then generated good yields purities cleavage respective under trifluoroacetic (TFA) dichloromethane (CH2Cl2).
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