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US 2023/0234973 A1Published application
Intermediate, preparing method thereof, and method of preparing drug
AssigneeHeron Neutron Medical Corp.
InventorsTeng-San Hsieh, Yu-Hou Yu, Tzung-Yi Lin
Life of this patent
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Abstract
An intermediate is provided herein, and it has the structure shown in the formula (1) as follows: formula (1). In the formula (1), R1 is —Cl, —Br, —I, —OSO2CF3, —B(OH)2, or R2 is —F, —18F, —Cl, —Br, —I, —SnMe3, —SnBu3, —B(OH)2, or and A is a chiral auxiliary.
Claims17
An intermediate, having a structure shown in formula (1) as follows:
- formula (1), wherein R1 is —Cl, —Br, —I, —OSO2CF3, —B(OH)2, or
- R2 is —F, —18F, —Cl, —Br, —I, —SnMe3, —SnBu3, —B(OH)2, or
- and A is a chiral auxiliary.
A method of preparing an intermediate, comprising:
- reacting a first reactant with a second reactant under an alkaline environment to obtain a first intermediate, a reaction temperature being from -80° C. to 0° C.,
- wherein the first reactant has a structure shown in formula (9-1) as follows:
- R3 is —Cl, —Br, —I, or —OSO2CF3-, R4 is —F, —Cl, —Br, —I, —SnMe3, —SnBus, or —B(OH)2, and X is —Br or —I;
- and
- the second reactant has a structure shown in formula (9-2) or formula (9-3), as follows:
- wherein A1 is a C1-C8 alkyl group, a C7-C10 aralkyl group, or a phenyl group, A2 is a C1-C8 alkyl group, and A3 is a C1-C8 alkyl group.
3 more elements
Dependencies are inferred from the claim text.