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US 12,747,217 B2Granted
Process for the manufacture of tetrazole derivatives
AssigneeHoffmann-La Roche Inc.
InventorsDainis Kaldre, Christian Oliver Kappe, Christian Steffen Moessner, Peter Sagmeister, Joerg Mathias Sedelmeier, Jason Douglas Williams
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Abstract
The present invention relates to a process for preparing a compound of formula (I), comprising reacting a compound of formula (II) with trimethylsilyl azide (TMSN3) and a chlorinating agent in acetonitrile, wherein the process is performed under continuous-flow conditions and wherein R1 and R2 are as defined in the description.
Claims19
A process for the preparation of a compound of formula (I)
- wherein
- R1 is alkyl, cycloalkyl, aryl, or arylalkyl;
- R2 is:
- —CH2—X;
- or aryl optionally substituted with one substituent independently selected from halogen, and alkoxy;
- or R1 and R2 together form alkylene;
- and
- X is halogen, aryloxy, alkyoxycarbonyl, or haloalkyl;
- comprising reacting a compound of formula (II)
- wherein R1 and R2 are as defined above;
- with trimethylsilyl azide (TMSN3) and POCl3 in acetonitrile under continuous-flow conditions.
8 more elements
Dependencies are inferred from the claim text.