71916-97-7

Upstream product

• 71916-95-5 1'-benzyl-5-chloro-2,3-dihydrospiro 
• 1003567-30-3 5-chloro-3H-spiro[1-benzofuran-2,4'-piperidine] hydrobromic acid salt 
• 3612-20-2 1-phenylmethyl-4-piperidone 
• 71916-91-1 5-chloro-2-fluorobenzyl bromide 
• 147804-30-6 1-oxa-6-aza-spiro-[2.5]octane-6-caboxylic acid tert-butyl ester 
• 1055710-50-3 C₁₇H₂₃ClFNO₃ 
• 1996-30-1 2-bromo-4-chloro-1-fluorobenzene 
• 644967-79-3 5-chlorospiro[1-benzofuran-2,4'-piperidine]-1'-carboxylic acid 1,1-dimethylethyl ester 
• 71916-92-2 1-benzyl-4-(5-chloro-2-fluorobenzyl)-4-piperidinol 

Downstream Products

• 1003567-11-0 5-chloro-2-{[(2S)-3-(5-chloro-3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-(p-methoxybenzyloxy)-N-methylbenzamide 
• 644968-71-8 N-(2-{[(2S)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-methoxyphenyl)acetamide 
• 644969-50-6 methyl 2-{[(2S)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-[(4-methoxybenzyl)oxy]benzoate 
• 644970-90-1 tert-butyl 2-{[(2S)-3-(5-chloro-1'H,3H-spiro[1-benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}benzoate 

Relevant academic research and scientific papers

Spirocyclic compounds, potent CCR1 antagonists

Conformationally constrained spirocycles (17-23) and (31-36) were synthesised. In vitro data revealed that these compounds are CCR1 antagonists with sub-nanomolar potency. In a functional assay 22, 23 and 36 inhibited CCR1 mediated chemotaxis with an ICs

PROCESS FOR THE PREPARATION OF CYCLIC SPIROPIPERIDINES

The present invention relates to new processes for the preparation of compounds of formula I, especially the compound 2-{2-Chloro-5-{[(2S)-3-(5-chloro-1'H,3H-spiro[1- benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-5 [(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid and to new intermediates useful in the preparation thereof.

A PROCESS FOR THE PREPARATION OF INTERMEDIATES AND THEIR US IN THE SYNTHESIS OF SPIROPIPERIDINE COMPOUNDS

The present invention relates to new processes for the preparation of compounds of formula I, especially the compound 2-{2-Chloro-5-{[(2S)-3-(5-chloro-1'H,3H-spiro[l- benzofuran-2,4'-piperidin]-1'-yl)-2-hydroxypropyl]oxy}-4-5[(methylamino)carbonyl]phenoxy}-2-methylpropanoic acid and to new intermediates useful in the preparation thereof.

NOVEL TRICYCLIC SPIROPIPERIDINE COMPOUNDS, THEIR SYNTHESIS AND THEIR USES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

Compounds of formula (I) wherein R1, R3, R4, R5, R6, R7, and R10 are as defined in the specification, are described. The present invention also relates to pharmaceutical composition comprising said compounds and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of said compounds and to new intermediates useful in the preparation thereof. Beside, the invention relates to salts and polymorphic forms of the new compounds as well as the preparation thereof.

NOVEL COMPOUNDS

The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, t, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their

NOVEL COMPOUNDS

The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, R3, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their prepa

NOVEL TRICYCLIC SPIRODERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

The invention provides compounds of formula (I) wherein m, R1, n, R2, q, p, X, Y, R3, R4, t and, R5 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

NOVEL TRICYCLIC SPIROPIPERIDINES OR SPIROPYRROLIDINES

The invention provides compounds of formula (I) wherein m, R1, n, R2, q, X, Y, Z, R3, R4, R5, R6, R7, R8, t and R9 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapy.

Synthesis of 2,3-Dihydrospiro and 2,3-dihydrospiro

The synthesis of 2,3-dihydrospiro 3 and 2,3-dihydrospiro 6 is described.The synthesis was achieved by a Grignard reaction of a 2-fluorobenzylhalide with an appropriate cycloazaalkyl ketone to yield