Parallel Synthesis of Drug-like 5-Amino-Substituted 1,2,4-Thiadiazole Libraries Using Cyclization Reactions of a Carboxamidine Dithiocarbamate Linker
DC Field | Value | Language |
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dc.contributor.author | Park, Joo Yeon | - |
dc.contributor.author | Ryu, In Ae | - |
dc.contributor.author | Park, Ji Hoon | - |
dc.contributor.author | Ha, Duck Chan | - |
dc.contributor.author | Gong, Young-Dae | - |
dc.date.accessioned | 2022-01-07T07:40:49Z | - |
dc.date.available | 2022-01-07T07:40:49Z | - |
dc.date.created | 2021-08-30 | - |
dc.date.issued | 2009-03-17 | - |
dc.identifier.issn | 0039-7881 | - |
dc.identifier.uri | https://scholar.korea.ac.kr/handle/2021.sw.korea/134699 | - |
dc.description.abstract | A general method has been developed for the solution-phase parallel synthesis of various drug-like 5-amino-substituted 1,2,4-thiadiazole derivatives, which employs initial cyclization reaction of carboxamidine dithiocarbamate 2 with p-toluenesulfonyl chloride. The carboxamidine dithiocarbamate 2 was produced by a three-component nucleophilic substitution reaction between carbon disulfide, benzamidine 1, and benzyl chloride. The key intermediate in this sequence, 5-(benzylsulfanyl)-3-phenyl-1,2,4-thiadiazole (3), is then transformed to the desired 5-amino-substituted 3-phenyl-1,2,4-thiadiazoles 6 in good yields and purities via oxidation of the sulfide group to form the corresponding sulfone followed by substitution reactions with various amines. | - |
dc.language | English | - |
dc.language.iso | en | - |
dc.publisher | GEORG THIEME VERLAG KG | - |
dc.subject | SOLID-PHASE SYNTHESIS | - |
dc.subject | SUBSTITUTED 1,3,4-THIADIAZOLES | - |
dc.subject | ANTICONVULSANT ACTIVITY | - |
dc.subject | ALLOSTERIC MODULATOR | - |
dc.subject | PDE4 INHIBITORS | - |
dc.subject | DERIVATIVES | - |
dc.subject | DESIGN | - |
dc.subject | 1,3,4-OXADIAZOLE | - |
dc.subject | SCH-202676 | - |
dc.subject | RECEPTORS | - |
dc.title | Parallel Synthesis of Drug-like 5-Amino-Substituted 1,2,4-Thiadiazole Libraries Using Cyclization Reactions of a Carboxamidine Dithiocarbamate Linker | - |
dc.type | Article | - |
dc.contributor.affiliatedAuthor | Ha, Duck Chan | - |
dc.identifier.doi | 10.1055/s-0028-1087970 | - |
dc.identifier.scopusid | 2-s2.0-67649427453 | - |
dc.identifier.wosid | 000264895300006 | - |
dc.identifier.bibliographicCitation | SYNTHESIS-STUTTGART, no.6, pp.913 - 920 | - |
dc.relation.isPartOf | SYNTHESIS-STUTTGART | - |
dc.citation.title | SYNTHESIS-STUTTGART | - |
dc.citation.number | 6 | - |
dc.citation.startPage | 913 | - |
dc.citation.endPage | 920 | - |
dc.type.rims | ART | - |
dc.type.docType | Article | - |
dc.description.journalClass | 1 | - |
dc.description.journalRegisteredClass | scie | - |
dc.description.journalRegisteredClass | scopus | - |
dc.relation.journalResearchArea | Chemistry | - |
dc.relation.journalWebOfScienceCategory | Chemistry, Organic | - |
dc.subject.keywordPlus | SOLID-PHASE SYNTHESIS | - |
dc.subject.keywordPlus | SUBSTITUTED 1,3,4-THIADIAZOLES | - |
dc.subject.keywordPlus | ANTICONVULSANT ACTIVITY | - |
dc.subject.keywordPlus | ALLOSTERIC MODULATOR | - |
dc.subject.keywordPlus | PDE4 INHIBITORS | - |
dc.subject.keywordPlus | DERIVATIVES | - |
dc.subject.keywordPlus | DESIGN | - |
dc.subject.keywordPlus | 1,3,4-OXADIAZOLE | - |
dc.subject.keywordPlus | SCH-202676 | - |
dc.subject.keywordPlus | RECEPTORS | - |
dc.subject.keywordAuthor | parallel synthesis | - |
dc.subject.keywordAuthor | drug-like properties | - |
dc.subject.keywordAuthor | 5-amino-1,2,4-thiadiazole | - |
dc.subject.keywordAuthor | dithiocarbamate linker | - |
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