WO2010054968 Quinazoline derivatives as NK3 receptor antagonists

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Scaffold: quinazoline

Biological target:

Neurokinin: NK-3

Activity:

antagonist

Steps Conditions Reactions
a

1. TBTU / DIEA / DMF

2. TFA / DCM

Amide synthesis (TBTU coupling) / Boc deprotection
b

DIEA / DMA

Tertiary amine synthesis (nucleophilic substitution)
Steps Conditions Reactions
a

1. n-BuLi / DIEA / THF

2. HCl 4N / Dioxane

3. NaOH aq

Nucleophilic substitution / Boc deprotection / Carboxylic acid synthesis (Ester hydrolysis)
b

DIEA / DMA

Tertiary amine synthesis (nucleophilic substitution)

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