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1.
J Org Chem ; 84(8): 4735-4747, 2019 04 19.
Article in English | MEDLINE | ID: mdl-30352146

ABSTRACT

A multidisciplinary approach covering synthetic, physical, and analytical chemistry, high-throughput experimentation and experimental design, process engineering, and solid-state chemistry is used to develop a large-scale (kilomole) Suzuki-Miyaura process. Working against clear criteria and targets, a full process investigation and optimization package is described highlighting how and why key decisions are made in the development of large-scale pharmaceutical processes.


Subject(s)
Drug Design , Drug Industry , Pyrazines/chemical synthesis , Triazines/chemical synthesis , High-Throughput Screening Assays , Molecular Structure , Pyrazines/chemistry , Triazines/chemistry
2.
Chem Commun (Camb) ; 52(46): 7368-71, 2016 May 31.
Article in English | MEDLINE | ID: mdl-26926388

ABSTRACT

A scalable, transferable, cooling crystallisation route to the elusive, metastable, form II of the API acetaminophen (paracetamol) has been developed using a multicomponent "templating" approach, delivering 100% polymorphic phase pure form II at scales up to 120 g. Favourable solubility and stability properties are found for the form II samples.

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