A concise route to MK-4482 (EIDD-2801) from cytidine
A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination of cytidine. The selective acylation and direct amination eliminate the need for protecting and activating groups and proceed in overall yield of 75%, a significant advancement over the reported yield of 17%. The step count is reduced from five transformations to two, and expensive uridine is replaced with the more available cytidine.
| Medienart: |
E-Artikel |
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| Erscheinungsjahr: |
2020 |
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| Erschienen: |
2020 |
| Enthalten in: |
Zur Gesamtaufnahme - volume:56 |
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| Enthalten in: |
Chemical communications (Cambridge, England) - 56(2020), 87 vom: 11. Nov., Seite 13363-13364 |
| Sprache: |
Englisch |
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| Beteiligte Personen: |
Vasudevan, N [VerfasserIn] |
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| Links: |
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| Themen: |
5CSZ8459RP |
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| Anmerkungen: |
Date Completed 14.05.2021 Date Revised 14.05.2021 published: Print-Electronic Citation Status MEDLINE |
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| doi: |
10.1039/d0cc05944g |
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| funding: |
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| Förderinstitution / Projekttitel: |
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| PPN (Katalog-ID): |
NLM31600555X |
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| 520 | |a A two-step route to MK-4482 (EIDD-2801, 1) was developed consisting of an esterification and hydroxamination of cytidine. The selective acylation and direct amination eliminate the need for protecting and activating groups and proceed in overall yield of 75%, a significant advancement over the reported yield of 17%. The step count is reduced from five transformations to two, and expensive uridine is replaced with the more available cytidine | ||
| 650 | 4 | |a Journal Article | |
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| 700 | 1 | |a Cardoso, Flavio S P |e verfasserin |4 aut | |
| 700 | 1 | |a Lucas, Tobias |e verfasserin |4 aut | |
| 700 | 1 | |a Dietz, Jule-Phillip |e verfasserin |4 aut | |
| 700 | 1 | |a Opatz, Till |e verfasserin |4 aut | |
| 700 | 1 | |a Jamison, Timothy F |e verfasserin |4 aut | |
| 700 | 1 | |a Gupton, Frank B |e verfasserin |4 aut | |
| 700 | 1 | |a Snead, David R |e verfasserin |4 aut | |
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