33107-83-4

Upstream product

• 186581-53-3 diazomethane 
• 25026-34-0 4-chlorophenacetyl chloride 
• 21443-38-9 1-(4-chlorophenyl)-3-diazo-propan-2-one 
• 1878-66-6 4-chlorophenylacetic Acid 
• 67442-07-3 2-chloro-N-methoxy-N-methylacetamide 
• 5586-88-9 1-(4-chlorophenyl)propan-2-one 
• 2549-51-1 vinyl chloroacetate 
• 96-34-4 methyl chloroacetate 
• 105-39-5 chloroacetic acid ethyl ester 

Downstream Products

• 56955-38-5 3-(4-chlorophenyl)-2-oxopropyl acetate 
• 924633-96-5 3-benzyloxy-2-(4-chloro-benzyl)-7,8,9,10-tetrahydro-benzo[h]quinoline-4-carboxylic acid benzyl ester 
• 851547-06-3 9-Benzyl-2-(4-chloro-benzyl)-3-hydroxy-7,8,9,10-tetrahydro-[1,9]phenanthroline-4-carboxylic acid 
• 851548-07-7 3-acetoxy-9-acetyl-2-(4-chloro-benzyl)-7,8,9,10-tetrahydro-[1,9]phenanthroline-4-carboxylic acid 
• 851547-04-1 2-(4-Chloro-benzyl)-3-hydroxy-9-isopropyl-7,8,9,10-tetrahydro-[1,9]phenanthroline-4-carboxylic acid 
• 851547-08-5 2-(4-Chloro-benzyl)-9-ethyl-3-hydroxy-7,8,9,10-tetrahydro-[1,9]phenanthroline-4-carboxylic acid 

Relevant academic research and scientific papers

A Simple and Efficient Method for the Preparation of α-Halogenated Ketones Using Iron(III) Chloride and Iron(III) Bromide as Halogen Sources with Phenyliodonium Diacetate as Oxidant

α-Halogenated ketones are both unique structure moieties existing in biologically natural products and valuable synthetic intermediates for the preparation of functional molecules. An efficient and scalable method for the preparation of α-halogenated ketone using iron (III) chloride and iron (III) bromide as halogen sources with phenyliodonium diacetate as oxidant has been developed, featuring mild reaction conditions, environmentally friendly reagents, and wide substrate scope. Notably, the three-step synthesis of drug prasugrel was achieved using this developed method as a key step with 30% yield on gram-scale. Additionally, the reaction mechanism involving chloride cation was proposed based on some preliminary control experiments. (Figure presented.).

One-step synthesis of 1-chloro-3-arylacetone derivatives from arylacetic acids

A practical one-step method has been developed to prepare α-chloroketones from readily available, inexpensive phenylacetic acid derivatives. The method utilizes the unique reactivity of an intermediate Mg.enolate dianion, which displays selectivity for the carbonyl carbon of chloromethyl carbonyl electrophiles. Decarboxylation of the intermediate occurs spontaneously during the reaction quench. The utility of the reaction products has been demonstrated through the total synthesis of the natural product cimiracemate B.

Methods and Compositions for Treatment of Scleritis and Related Disorders

The present teachings relate to the field of anti-inflammatory substances and more particularly to compounds that are useful for the treatment of scleritis, a scleritis symptom, or a scleritis-related disorder. In one aspect, methods of treating scleritis, a scleritis symptom, or a scleritis-related disorder generally include administering to a subject a compound of Formula I: or a pharmaceutically acceptable salt, hydrate or ester thereof, wherein W1, W2, R1, L, X, Y, Z, and n1 are defined as described herein.

2-(4-Chlorobenzyl)-3-hydroxy-7,8,9,10-tetrahydrobenzo[H] quinoline-4-carboxylic acid (PSI-697): Identification of a clinical candidate from the quinoline salicylic acid series of P-selectin antagonists

P-selectin-PSGL-1 interaction causes rolling of leukocytes on the endothelial cell surface, which subsequently leads to firm adherence and leukocyte transmigration through the vessel wall into the surrounding tissues. P-selectin is upregulated on the surface of both platelets and endothelium in a variety of atherosclerosis-associated conditions. Consequently, inhibition of this interaction by means of a small molecule P-selectin antagonist is an attractive strategy for the treatment of atherosclerosis. High-throughput screening and subsequent analoging had led to the identification of compound 1 as the lead candidate. Herein, we report the continuation of this work and the discovery of a second-generation series, the tetrahydrobenzoquinoline salicylic acids. These compounds have improved pharmacokinetic properties, and a number of them have shown oral efficacy in mouse and rat models of atherogenesis and vascular injury. The lead 31 (PSI-697), is currently in clinical development for the treatment of atherothrombotic vascular events.

METHOD FOR PRODUCING 1-HALO-3-ARYL-2-PROPANONE

1-halo-3-aryl-2-propanone can be produced with ease and with good efficiency without the use of a reagent being difficult to handle or the equipment for a super low temperature reaction, by using a method comprising reacting an enolate prepared from an arylacetic acid or an arylacetic acid derivative, which is inexpensive and easily available, and a base, with a haloacetic acid derivative, which is inexpensive and easily available, followed by the treatment with an acid. 1-halo-3-aryl-2-propanone is useful as a pharmaceutical intermediate or the like.

Methods and compositions for selectin inhibition

The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated disorders are provided which include administration of compound of Formula I: wherein the constituent variables are defined herein.

Methods and compositions for selectin inhibition

The present invention relates to the field of anti-inflammatory substances, and more particularly to novel compounds that act as antagonists of the mammalian adhesion proteins known as selectins. In some embodiments, methods for treating selectin mediated

ISOXAZOLE AND PYRAZOLE DERIVATIVES AS DOPAMINE RECEPTOR SUBTYPE LIGANDS

A class of substituted isoxazole and pyrazole derivatives of formula (I), or a salt thereof of or a prodrug thereof, wherein the broken circle represents two non-adjacent double bonds whereby the five-membered ring containing X and Y is aromatic; one of X and Y represents nitrogen, and the other of X and Y represents oxygen or N--R 5 ; R. sup.1 represents hydrogen, C 1-6 alkyl or trifluoromethyl; R 2 and R 3 independently represent hydrogen, hydrocarbon, a heterocyclic group, halogen, cyano, trifluoromethyl, nitro,--OR a,--SR a,--SOR a,--SO 2 R a,--SO 2 NR. sup.a R b,--NR a R. sup.a,--NR a CO 2 R b,--COR a,--CO 2 R a or--CONR a R b, R 4 represents hydrocarbon or a heterocyclic group; R 5 represents hydrogen or C 1-6 alkyl; and R a and R. sup.b independently represent hydrogen, hydrocarbon or a heterocyclic group, are ligands for dopamine receptor subtypes within the body and are therefore useful in the treatment and/or prevention of disorders of the dopamine system, in particular schizophrenia. STR1