762286-32-8

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 144043-17-4 (3R)-1-benzyl-N-methylpyrrolidin-3-amine 
• 865-47-4 potassium tert-butylate 
• 77-78-1 dimethyl sulfate 
• 131878-23-4 (3R)-1-benzyl-3-[(tert-butoxycarbonyl)(methyl)amino]pyrrolidine 

Downstream Products

• 1313412-63-3 (R)tert-butyl 1-(2-amino-6-(benzyloxymethyl)pyrimidin-4-yl)pyrroIidin-3yl(methyl)carbamate 
• 392338-15-7 tert-butyl [(3R)-pyrrolidin-3-yl]methylcarbamate 

Relevant academic research and scientific papers

Development of the Late-Phase Manufacturing Process of ZPL389: Control of Process Impurities by Enhanced Process Knowledge

The development of the late-phase manufacturing process of the drug candidate ZPL389 and the strategies for the control of impurities are outlined in detail. Selective salt formation at several stages was pivotal to controlling the process impurities. The extensive optimization of the N-methylation of a Boc-protected amine with dimethyl sulfate and of a nucleophilic aromatic substitution without the use of metal catalysts led to a robust, scalable process. The process was demonstrated on a >100 kg scale. Overall, improved drug substance quality, higher yield, and reduction of the process mass intensity were achieved.

AMINOALKYLPYRIMIDINE DERIVATIVES AS HISTAMINE H4 RECEPTOR ANTAGONISTS

Aminoalkyipyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

2H-PYRAZOLO [4,3-D]PYRIMIDIN-5-AMINE DERIVATIVES AS H4 HISTAMINE RECEPTOR ANTAGONISTS FOR THE TREATMENT OF ALLERGIC, IMMUNOLOGICAL AND INFLAMMATORY DISEASES

Pyrazolopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

PIPERIDIN-PYRIMIDINE DERIVATIVES AS ANTAGONISTS OF HISTAMINE H4 RECEPTOR

Piperidin-pyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

FURO[3,2-D]PYRIMIDINE DERIVATIVES

Furo[3,2-d]pyrimidine derivatives of formula I, wherein the meanings for the various substituents are as defined in the description. These compounds are useful as H4 receptor antagonists.

2 -AMINOPYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS

2-Amino-pyrimidine derivatives of formula I, wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine receptor H4antagonists.

4-AMINO-PYRIMIDINE DERIVATIVES

4-Amino-pyrimidine derivatives of Formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

2 -AMINO-PYRIMIDINE DERIVATIVES AS HISTAMINE H4 ANTAGONISTS

2-Aminopyrimidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

FURO [3, 2-D] PYRIMIDINE DERIVATIVES AS H4 RECEPTOR ANTAGONISTS

Furo[3,2-d]pypnnidine derivatives of formula (I), wherein the meaning of the different substituents are those indicated in the description. These compounds are useful as histamine H4 receptor antagonists.

Macrocyclic Spiro Pyrimidine Derivatives

Macrocyclic spiro pyrimidine compounds, compositions comprising such compounds, methods for making the compounds, and methods of treating and preventing the progression of diseases, conditions, and disorders using such compounds and compositions are described herein.