Recent advances in traceless linkers

Current Opinion in Drug Discovery and Development

Volumn 2, Issue 4, 1999, Pages 358-364

  Reitz, Allen B ^a  

^a R W JOHNSON PHARMACEUTICAL RES I   (United States)

Author keywords

Compound libraries; Resin; Solid phase synthesis; Traceless linkers

Indexed keywords

BENZODIAZEPINE DERIVATIVE; CHROMIUM DERIVATIVE; RESIN;

ARTICLE; CHEMICAL REACTION; CYCLIZATION; DRUG SYNTHESIS; REDUCTION;

EID: 0032800168     PISSN: 13676733     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (50)

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9. •Anchimeric assistance greatly enhances the rate of protodesilation.
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14. •The iriazene linker method for attaching aromatic substrates is versatile and the resin can be regenerated upon cleavage. There are many suitable anilines which could be considered as starting materials for coupling to the resin.
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16. This interesting chemistry is limited by the relatively severe conditions required for cleavage. Alkylsulfonate esters would be easier to cleave based on the similar reactivity observed in reductions ofmesyl groups.
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24. •Decarboxylation, as described in this paper, could be used in a variety of other related applications.
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40. •This versatile procedure can be further enhanced by the development and availability of a variety of sulfonyl chloride resins with complementary reactivities.
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43. This was the first example of the sulfonate ester displacement procedure.
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46. •This is a very useful method and has been applied broadly in different laboratories.
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49. This is an innovative approach which can be extended to other related organometallic systems.
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