Le Grand, Darren Mark et al. published their patent in 2003 |CAS: 490021-97-1

The Article related to azetidine preparation ccr3 receptor antagonist, Heterocyclic Compounds (One Hetero Atom): 4-Membered Rings and other aspects.SDS of cas: 490021-97-1

On September 25, 2003, Le Grand, Darren Mark; McCarthy, Clive; Walker, Clive Victor; Woods, John James published a patent.SDS of cas: 490021-97-1 The title of the patent was Preparation of azetidine derivatives as CCR-3 receptor antagonists. And the patent contained the following:

The title compounds [I; Ar = (un)substituted Ph; R1 = H, alkyl optionally substituted by OH, alkoxy, acyloxy, halo, CO2H, etc.; R2 = H, alkyl or cycloalkyl, and R3 = alkyl substituted by Ph, OPh, acyloxy or naphthyl, or R3 = cycloalkyl optionally having a benzo group fused thereto, a heterocyclic group having 5-11 ring atoms of which 1-4 are heteroatoms, (un)substituted Ph or naphthyl, or R2 and R3 together with the nitrogen atom to which they are attached denote a heterocyclic group having 5-10 ring atoms of which 1-3 are heteroatoms; X = CO, O, CH2, CH(OH); Y = O, S; m = 1-4; and n, p and q = 0, 1 (n+p+q = 1, 2; n+q = 1; p+q = 1; and when n = 0, p = 0)], useful for treating conditions mediated by CCR3, were prepared Thus, reacting (S)-2-amino-4-[3-(4-chlorophenoxy)azetidin-1-yl]butan-1-ol with 3,5-dimethoxyphenyl isocyanate in CH2Cl2 afforded the urea (S)-II which showed IC50 of 0.007 μM against CCR-3 binding. The exemplified compounds I generally have IC50 values below 1 μM in CCR-3 binding assay. Pharmaceutical compositions that contain the compounds I and processes for preparing the compounds are also described. The experimental process involved the reaction of 3-(4-Chlorophenoxy)azetidine hydrochloride(cas: 490021-97-1).SDS of cas: 490021-97-1

The Article related to azetidine preparation ccr3 receptor antagonist, Heterocyclic Compounds (One Hetero Atom): 4-Membered Rings and other aspects.SDS of cas: 490021-97-1

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics