Amido compound and its application as medicine
A technology for compounds and medicinal salts, applied in the field of modulators of type 1 11-beta hydroxysteroid dehydrogenase and/or mineralocorticoid receptors, can solve problems such as increasing the risk of fractures
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[0224] The preparation of compounds involves the protection and deprotection of various chemical groups. The selection of protection and deprotection as well as the selection of suitable protecting groups can be easily determined by those skilled in the art. Protecting group chemistry can be found in, for example, Greene, et al., Protective Groups in Organic Synthesis, Second Edition, Wiley & Sons, 1991, which is incorporated herein by reference in its entirety.
[0225] The reaction of the method described herein can be carried out in a suitable solvent, which can be easily selected by those skilled in the art of organic synthesis. At the temperature at which the reaction proceeds, that is, from the freezing temperature of the solvent to the boiling temperature of the solvent, a suitable solvent does not substantially react with the starting materials (reactants), intermediates or products. A given reaction can be carried out in one solvent or a mixture of more than one solvent...
Embodiment 1
[0338] (3S)-1-((1-(4-chlorophenyl)cyclopropyl)carbonyl)pyrrolidin-3-ol
[0339] To 1-(4-chlorophenyl) cyclopropanecarboxylic acid (50mg, 0.25mmol), (3S)-pyrrolidin-3-ol (24.4mg, 0.28mmol) and BOP (116.0mg, 0.26mmol) in 0.4mL DMF In the solution inside, add hunig base (0.066ml, 0.38mmol). The mixture was stirred at room temperature overnight, and then directly purified by preparative HPLC to obtain (3S)-1-((1-(4-chlorophenyl)cyclopropyl)carbonyl)pyrrolidin-3-ol (20 mg). LCMS: m / z266.0(M+H) + 553.1(2M+Na) + .
Embodiment 2
[0341] (3S)-1-[(1-phenylcyclopropyl)carbonyl]pyrrolidin-3-ol
[0342] This compound was prepared by a method similar to that described in Example 1. LCMS: m / z232.1(M+H) + .
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