Bivalent linkers and conjugates thereof
US-9090563-B2 · Jul 28, 2015 · US
US9505747B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9505747-B2 |
| Application number | US-201314388311-A |
| Country | US |
| Kind code | B2 |
| Filing date | Mar 29, 2013 |
| Priority date | Mar 29, 2012 |
| Publication date | Nov 29, 2016 |
| Grant date | Nov 29, 2016 |
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The invention described herein pertains to processes for preparing tubulysin derivatives, conjugates of tubulysins, and intermediates therefore. In one illustrative embodiment of the invention, processes for derivatives or analogs of natural tubulysins including compounds of formula (T). In another embodiment, vitamin receptor binding conjugates of tubulysins are described. The processes include one or more steps described herein. In another embodiment, a process is described for preparing a compound of formula B, wherein R5 and R6 are as described in the various embodiments herein, such as each being independently selected from optionally substituted alkyl or optionally substituted cycloalkyl; and R8 is C1-C6 n-alkyl; wherein the process comprises the step of treating a compound of formula A with a silylating agent, such as triethylsilyl chloride, and a base, such as imidazole in an aprotic solvent.
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What is claimed is: 1. A process for preparing a compound of the formula or a salt or solvate thereof; wherein Ar 1 is optionally substituted aryl or optionally substituted heteroaryl; Ar 2 is optionally substituted aryl or optionally substituted heteroaryl; L is selected from the group consisting of…
Chemistry & Metallurgy · mapped topic
Chemistry & Metallurgy · mapped topic
Chemistry & Metallurgy · mapped topic
Chemistry & Metallurgy · mapped topic
Chemistry & Metallurgy · mapped topic
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