16323-08-3

Upstream product

• 446-08-2 2-amino-5-fluorobenzoic acid 
• 2466-76-4 N-Acetylimidazole 
• 53981-24-1 2-amino-5-fluorophenol 
• 446-36-6 5-fluoro-2-nitrophenol 
• 108-24-7 acetic anhydride 

Downstream Products

• 137589-57-2 N-(4-fluoro-2-hydroxy-5-nitrophenyl)acetamide 
• 460047-96-5 N-{4-Fluoro-2-[(2S)oxiranylmethoxy]phenyl}acetamide 
• 1021860-56-9 (7-fluoro-3,4-dihydro-2H-1,4-benzoxazin-3-yl)methanol 
• 1021860-55-8 (7-fluoro-3,4-dihydro-2H-1,4-benzoxazin-3-yl)methyl acetate 
• 384346-15-0 N-{4-fluoro-2-[(2S)-oxiran-2-ylmethoxy]phenyl}acetamide 

Relevant academic research and scientific papers

De Novo Biosynthesis and Whole-Cell Catalytic Production of 2-Acetamidophenol in Escherichia coli

2-Acetamidophenol (AAP) is an aromatic product with promising activities in agricultural applications and medical research. At present, AAP is synthesized by chemical methods from nonrenewable fossil fuel resources, which cause environmental pollution and the reaction conditions are harsh. In this study, we constructed the artificial biosynthetic pathway of AAP with five different expressed proteins in Escherichia coli for the first time. By introducing the hydrogen peroxide degrading enzyme catalase and improving cell tolerance to toxic intermediates or products, the yield of AAP reached 33.54 mg/L using shaking-flask culture. The best-engineered strain could produce 568.57 mg/L AAP by fed-batch fermentation from glucose and precursor (2-aminophenol, 2-AP) addition. Furthermore, a one-pot whole-cell cascade biocatalytic pathway to AAP and analogues was developed and optimized. This method can efficiently produce 1.8 g/L AAP using the methyl anthranilate hydrolysis product as the substrate. This study provides not only the de novo artificial biosynthetic pathway of AAP in E. coli but also a promising sustainable and efficient strategy to enable the synthesis of AAP on a gram scale.

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

BENZOXAZINE DERIVATIVES AND USES THEREOF

Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided, wherein each of Z, X, R1, R2, R3, R4, y, n, and Ar are as defined, and described in classes and subclasses herein, which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions thereof, are useful for treating a variety of central nervous system disorders such as schizophrenia.

NOVEL TRICYCLIC SPIRODERIVATIVES AS MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY

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, proc

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.

Process and intermediates for the preparation of substituted 6-(3,5,6,7-tetrahydropyrrolo-[2,1-c][1,2,4]-thiadiazol-3-ylidenimino)-7-fluoro-2H-1,4-benzoxazin-3(4H)-ones

The invention relates a new process for the preparation of substituted 6-(3,5,6,7-tetrahydropyrrolo[2,1-c][1,2,4]-thiadiazol-3-ylidenimino)-7-fluoro-2H-1,4-benzoxazin-3(4H)-ones of general formula I in which, R1 is C1-C6-alkyl, Csub