An Alternative Focus for Route Design for the Synthesis of Antibody-Drug Conjugate Payloads.
J Org Chem
; 84(8): 4830-4836, 2019 04 19.
Article
em En
| MEDLINE
| ID: mdl-30602115
ABSTRACT
An analysis of Antibody-Drug Conjugate Payload manufacturing has revealed that the majority of the cost is associated with the use of high-containment facilities for the latter stages of the synthesis. To make a significant reduction in the Cost of Goods (CoGs), a new approach to route design has been introduced which focuses on minimizing the number of steps that require high containment. This approach has been exemplified in a new synthesis of tesirine, including the first application of a ring-closing copper(I)/TEMPO aerobic oxidation to the pyrrolobenzodiazepine ring system, affording a 60% reduction in CoGs.
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1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Pirróis
/
Benzodiazepinas
/
Desenho de Fármacos
/
Imunoconjugados
Idioma:
En
Revista:
J Org Chem
Ano de publicação:
2019
Tipo de documento:
Article