787564-48-1

Upstream product

• 478385-97-6 (2S)-1-benzoyl-2-fluoromethylpyrrolidine 
• 91599-81-4 (R)-N-benzyl-3-hydroxypiperidine 
• 53912-80-4 (S)-N-benzylprolinol 

Downstream Products

• 787564-37-8 (3R)-3-fluoropiperidine hydrochloride 
• 787564-55-0 (S)-2-(fluoromethyl)pyrrolidine hydrochloride 

Relevant academic research and scientific papers

Nucleophilic fluorination of amino alcohols and diols using deoxofluor

Various fluorinated chiral compounds were synthesized using bis(2-methoxyethyl)aminosulfur trifluoride (Deoxofluor) as a nucleophilic fluorinating reagent. Reactions of Deoxofluor (1) with amino alcohols (2a-d) and diols (2e-g) in methylene chloride at room temperature led to the formation of the corresponding fluoro derivatives (3a-g) in good yields.

Ring expansion induced by DAST: Synthesis of substituted 3-fluoropiperidines from prolinols and 3-fluoroazepanes from 2-hydroxymethylpiperidines

Optically active prolinols can be converted into optically active 3-fluoropiperidines by treatment with DAST. The reaction often produces 2-fluoromethylpyrrolidines as byproducts. The ring expansion was also applied to 2-hydroxypiperidines to produce 3-fl

Synthesis of optically active substituted 3-fluoropiperidines from prolinols by using DAST

The treatment of optically active prolinols with DAST produces optically active 3-fluoropiperidines via aziridinium intermediates. Georg Thieme Verlag Stuttgart.

PYRAZOLE DERIVATIVE

A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

1,5-DIHETEROCYCLE-1H-TRIAZOLE DERIVATIVE

The present invention relates to a compound represented by Formula (I): wherein Ar1, Ar2, R1 and R2 each represent a substituent, a salt thereof, or a solvate of the compound or the salt, and to a medicine containing the same. According to the present invention, a potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.

PYRAZOLE DERIVATIVES

A compound represented by formula (I): (wherein Ar1 represents a phenyl group which may have 1 to 3 substituents, or a non-substituted 5- or 6-membered aromatic heterocyclic group; Ar2 represents (i) a non-substituted phenyl group, (ii) a phenyl group which has been substituted by a lower alkyl group having 1 to 3 groups or atoms selected from among a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom, or (iii) a 5- or 6-membered nitrogen-containing aromatic heterocyclic group which has been substituted by 1 to 3 groups or atoms selected from among a lower alkyl group, a lower alkynyl group, a lower alkanoyl group, a carbamoyl group, a cyano group, an amino group, a hydroxyl group, a lower alkoxy group, and a halogen atom; and X represents a group represented by formula (II): (wherein the ring structure represents a 4- to 7-membered heterocyclic group which may have, in addition to the nitrogen atom shown in formula (II), one heteroatom selected from among nitrogen, oxygen, and sulfur, and which may be substituted by 1 to 4 groups or atoms selected from among a lower alkyl group, a carbamoyl group, an amino group, a hydroxyl group, a lower alkoxy group, an oxo group, a lower alkanoyl group, a lower alkylsulfonyl group, and a halogen atom)), a salt thereof, a solvate of the compound or the salt, and a drug.

FIVE-MEMBERED HETEROCYCLIC DERIVATIVE

The present invention relates to a compound represented by formula (I): a salt of the compound, or a solvate of the compound or the salt; a drug containing any of the compounds, the salts, and the solvates; a preventive and/or therapeutic agent for an ischemic disease containing any of the compounds, the salts, and the solvates; and a platelet coagulation inhibitor containing any of the compounds, the salts, and the solvates. The compound of the present invention is useful as a strong platelet coagulation inhibitor without inhibiting COX-1 or COX-2.

Rearrangements accompanying fluorination of 2-amino alcohols and 1,2-diols with Deoxo-Fluor

2-Amino alcohols and 1,2-diols treated with Deoxo-Fluor in methylene chloride resulted in the formation of rearranged major products concomitantly with minor amounts of the straightforward fluorinated replacement products in good yields.