19722-96-4Relevant academic research and scientific papers
New synthetic uses of 2,3-dihydro-3-oxobenzo[b]thiophene
Deprets, Stephanie,Jarkas, Nachwa,Kirsch, Gilbert
, p. 401 - 402 (1999)
Synthesis of benzo[b]thiophenes functionalized in the position 3 and new polycyclic systems are discussed.
COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0314; 0485; 0486, (2018/02/27)
Compounds of formula (I) wherein: Ak1 represents an alkyl chain, X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)—, —N(R)—CH2— or —CH2—N(R)—CH2—, m and R are as defined in the description, R1 and R2 each represent H when X represents —(CH2)m—, —CH(R)—, —N(R)—, —CH2—N(R)— or —N(R)—CH2—, or together form a bond when X represents —CH2—N(R)—CH2—, R3 represents NH2, Cy-NH2, Cy-Ak3-NH2 or piperidin-4-yl, Cy and Ak3 are as defined in the description, R4 and R5, which may be identical or different, each represent H or F, their optical isomers, and addition salts thereof with a pharmaceutically acceptable acid. Medicinal products containing the same which are useful in treating conditions requiring a TAFIa inhibitor.
Transient-Ligand-Enabled ortho-Arylation of Five-Membered Heterocycles: Facile Access to Mechanochromic Materials
Li, Bijin,Seth, Kapileswar,Niu, Ben,Pan, Lei,Yang, Huiwen,Ge, Haibo
supporting information, p. 3401 - 3405 (2018/02/28)
Reported herein is the first example of a direct arylation of heteroarenes by a transient-ligand-directed strategy without the need to construct and deconstruct the directing group. A wide range of heteroarenes undergoes the coupling with diverse aryl iod
NEW BICYCLIC THIOPHENYLAMIDE COMPOUNDS
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Page/Page column 71; 72, (2014/01/09)
The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, A, E and n are as described herein, compositions including the compounds and use thereof as fatty-acid binding protein (FABP) 4/5 inhibitors in the treatment of e.g. type 2 diabetes, atherosclerosis or cancer.
Microwave-assisted syntheses of N-heterocycles using alkenone-, alkynone- and aryl-carbonyl O-phenyl oximes: Formal synthesis of neocryptolepine
Portela-Cubillo, Fernando,Scott, Jackie S.,Walton, John C.
, p. 5558 - 5565 (2008/12/20)
(Chemical Equation Presented) This research aimed to provide a new and "clean" synthetic method that would enable both known and novel N-heterocycles to be prepared efficiently. O-Phenyl oximes were found to be excellent precursors for iminyl radicals with a variety of acceptor side chains. Dihyropyrroles were made in good yields from O-phenyl oximes containing pent-4-ene acceptors. The analogous process with a hex-5-enyl acceptor did not yield a dihydropyridine, probably because the 6-exo-trig ring closure of the iminyl radical was too slow to compete with H-atom abstraction. The iminyl radical from a precursor with a pent-4-yne type side chain underwent ring closure followed by rearrangement to afford a pyrrole derivative. Suitably substituted iminyl radicals ring closed readily onto aromatic acceptors, thus enabling several polycyclic systems to be accessed. Quinolines were made from 3-phenylpropanones via their O-phenyl oximes. Syntheses of phenanthridines starting from 2-formylbiphenyls were particularly efficient, and this approach enabled the natural product trisphaeridine to be made. Starting from 2-phenylnicotinaldehyde derivatives, ring closures of the derived iminyl radicals onto the phenyl rings yielded benzo[h][1,6]naphthyridines. Similarly, ring closure onto a phenyl ring from a benzothiophene-based iminyl yielded a benzo[b-]thieno[2,3-c]quinoline. By way of contrast, iminyl radical ring closure onto pyridine rings was not observed. However, iminyl radicals did cyclize onto indoles, enabling indolopyridines to be prepared. The latter route was exploited in a short formal synthesis of neocryptolepine starting from 2-((1H-indol-3-yl)methyl)cyclohexanone.
Synthesis of 5-methylbenzo[b]thieno[2,3-c]isoquinolines and 5- methylbenzo[b]seleno[2,3-c]isoquinolines
Deprets, Stephanie,Kirsch, Gilbert
, p. 1353 - 1357 (2007/10/03)
5-Methylbenzo[b]thieno[2,3-c]isoquinolines and 5- methylbenzo[b]seleno[2,3-c]isoquinolines 11b,c have been prepared by Bischler-Napieralski cyclization of 2-acetamido-3-phenylbenzo[b]heteroarenes.
Method for treating diarrhea with benzothiophene derivatives
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, (2008/06/13)
Compounds of the formula: STR1 and pharmaceutically-acceptable acid addition salts thereof, wherein R1 is at the 3 or 4 position and is phenyl or phenyl substituted by halo, (C1 -C4)alkoxy, or (C2 -C5
PHOTOCYCLOADDITIONS TO 3-PHENYL-1,2-BENZISOTHIAZOLE
Sindler-Kulyk, M.,Neckers, D. C.
, p. 529 - 532 (2007/10/02)
3-Phenyl-1,2-benzisothiazole (1) gave upon irradiation in the presence of ethyl vinyl ether 3-ethoxy-5-phenyl-2,3-dihydro-1,4-benzosothiazepine (II) in high yield (80percent).
PHOTOCYCLOADDITIONS TO 3-PHENYL-1,2-BENZISOTHIAZOLE
Sindler-Kulyk, M.,Neckers, D. C.,Blount, J. R.
, p. 3377 - 3384 (2007/10/02)
Photocycloaddition reactions of 3-phenyl-1,2-benzisothiazole to alkenes yield derivatives of 2,3-dihydro-1,4-benzothiazepine in one step reactions.The photoadditions are both regio and stereospecific.
