176526-00-4Relevant articles and documents
A route to dihydro[2]benzooxepino[4,5-c]pyridines and dihydrothieno[d][2]benzooxepines via the 1.7-electrocyclisation of carbonyl ylides
O'Shea, Donal F.,Sharp, John T.
, p. 515 - 518 (1996)
The cyclisation of diene-conjugated carbonyl ylides of the general type 2, in which the α,β; γ,δ diene function is formed by a benzene ring and either a thiophene or pyridine ring provides a new route to some hetero-fused dihydrobenzooxepines. The oxirane
COMPOUNDS OF PHOSPHINANES AND AZAPHOSPHINANES, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM
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Paragraph 0314; 0426; 0427, (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.
Intramolecular Acylation of Unactivated Pyridines or Arenes via Multiple C-H Functionalizations: Synthesis of All Four Azafluorenones and Fluorenones
Laha, Joydev K.,Jethava, Krupal P.,Patel, Sagarkumar,Patel, Ketul V.
, p. 76 - 85 (2017/04/26)
An unprecedented intramolecular acylation of unactivated pyridines via multiple C(sp3/sp2)-H functionalizations of a methyl, hydroxymethyl, or aldehyde group has been developed providing a general access to all four azafluorenones. The application of this protocol is further demonstrated to the synthesis of azafluorenone related fused nitrogen heterocycles and fluorenones. In addition, design and synthesis of a novel fluorene based organic emitter for potential use in organic light emitting devices (OLEDs) is also reported.
Silver-Catalyzed Tandem C=C Bond Hydroazidation/Radical Addition/Cyclization of Biphenyl Acetylene: One-Pot Synthesis of 6-Methyl Sulfonylated Phenanthridines
Tang, Jiawei,Sivaguru, Paramasivam,Ning, Yongquan,Zanoni, Giuseppe,Bi, Xihe
supporting information, p. 4026 - 4029 (2017/08/14)
A silver-catalyzed tandem carbon-carbon triple bond hydroazidation, radical addition, and cyclization of biphenyl acetylene is described under mild conditions, leading to the formation of 6-methyl sulfonylated phenanthridines in good yields. In this novel cascade reaction, most of the atoms are incorporated into the product without cleavage of the C=C bond. Mechanistic studies suggest the reaction should proceed through an iminyl radical reactive intermediate.
Phosphine-Free Suzuki Cross-Coupling Reaction Using an Efficient and Reusable Pd Catalyst in an Aqueous Medium under Microwave Irradiation
Da Silva, Joaquim F. M.,Yepes Perez, Andres F.,De Almeida, Natália P.
supporting information, p. 1995 - 2004 (2015/08/18)
We report here an improved, highly efficient, and general method for the ligand-free Suzuki cross-coupling reaction to the synthesis of biaryls, bipyridyls, thienylpyridine, and allylphenols. Microwave irradiation of (het)aryl halides and (hetaryl, allyl)arylboronic acid N-methyl-iminodiacetic acid (MIDA) ester, using polyurea microencapsulated palladium catalyst (Pd EnCat 30), gave the coupling adducts 1a-x in excellent yields in just 10-18 min.
A new synthetic approach to 6-unsubstituted phenanthridine and phenanthridine-like compounds under mild and metal-free conditions
Tummatorn, Jumreang,Krajangsri, Suppachai,Norseeda, Krissada,Thongsornkleeb, Charnsak,Ruchirawat, Somsak
supporting information, p. 5077 - 5081 (2014/07/08)
A new and mild synthetic approach for the synthesis of 6-unsubstituted phenanthridine and phenanthridine-like compounds under metal-free conditions at room temperature has been developed. The strategy involved a tandem azide rearrangement/intramolecular annulation and oxidation reactions of biarylmethyl azide precursors to obtain the desired products in up to 99% yields with high regioselectivity.
Synthesis of phenanthrenes through copper-catalyzed cross-Coupling of N-tosylhydrazones with terminal alkynes
Hossain, Mohammad Lokman,Ye, Fei,Liu, Zhenxing,Xia, Ying,Shi, Yi,Zhou, Lei,Zhang, Yan,Wang, Jianbo
, p. 8689 - 8699 (2015/01/08)
A novel protocol for the synthesis of phenanthrenes through the copper-catalyzed reaction of aromatic tosylhydrazones with terminal alkynes is explored. The reaction proceeds via the formation of an allene intermediate and subsequent six-π-electron cyclization-isomerization, affording phenanthrene derivatives in good yields. The transformation can be performed in two ways:(1)with Ntosylhydrazones derived from [1,1'-biphenyl]-2-carbaldehydes and terminal alkynes as the starting materials and(2)with Ntosylhydrazones derived from aromatic aldehydes and 2-alkynyl biphenyls as the starting materials. This new phenanthrene synthesis uses readily available starting materials and a cheap copper catalyst and has a wide range of functional group compatibility.
An efficient and new protocol for phosphine-free Suzuki coupling reaction using palladium-encapsulated and air-stable MIDA boronates in an aqueous medium
Mendes Da Silva, Joaquim Fernando,Yepes Perez, Andres Felipe,Pinto De Almeida, Natalia
, p. 28148 - 28155 (2014/07/21)
A simple methodology that uses a system based on polyurea microencapsulated palladium (PdEnCat 30) and aryl or (2-pyridyl) MIDA boronates for Suzuki-Miyaura cross-coupling reactions of (hetero)aryl halides in water-alcohol under phosphine-free conditions was developed. This journal is the Partner Organisations 2014.
Expeditious synthesis of phenanthrenes via CuBr2-catalyzed coupling of terminal alkynes and N-tosylhydrazones derived from O-formyl biphenyls
Ye, Fei,Shi, Yi,Zhou, Lei,Xiao, Qing,Zhang, Yan,Wang, Jianbo
supporting information; experimental part, p. 5020 - 5023 (2011/11/14)
A new method for the synthesis of phenanthrenes via ligand-free CuBr2-catalyzed coupling/cyclization of terminal alkynes with N-tosylhydrazones derived from o-formyl biphenyls has been developed. This new synthesis has wide range of functional group compatibility.
NOVEL CURCUMIN DERIVATIVE
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Page/Page column 106, (2009/12/07)
The present invention provides a novel compound that is structurally similar to curcumin and has a suppressive effect on Aβ aggregation, a degradative effect on Aβ aggregates, an inhibitory effect on β-secretase, and a protective effect on neurons. The novel compound is a compound represented by the following general formula (Ia) or a salt thereof: wherein R1 represents a 4-hydroxy-3-methoxyphenyl group or the like, and R2 represents a 1H-indol-6-yl group or the like.
