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Discovery and SAR of potent, orally available and brain-penetrable 5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen- and 4,5-dihydro-6-oxa-3-thia-1-aza- benzo[e]azulen derivatives as neuropeptide Y Y5 receptor antagonists

Combination of structural elements from a potent Y5 antagonist (2) with thiazole fragments that exhibit weak Y5 affinities followed by lead optimisation led to the discovery of (5,6-dihydro-4H-3-thia-1-aza-benzo[e]azulen-2-yl)- piperidin-4-ylmethyl-amino and (4,5-dihydro-6-oxa-3-thia-1-aza-benzo[e]azulen-2- yl)-piperidin-4-ylmethyl-amino derivatives. Both classes of compounds are capable of delivering potent and selective orally and centrally bioavailable NPY Y5 receptor antagonists.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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MTHFD2 INHIBITORS AND USES THEREOF

The present invention provides compounds, compositions thereof, and methods of using the same.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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MELANOCORTIN RECEPTOR AGONISTS

The present invention relates to a compound having a good agonistic activity to melanocortin receptor, or pharmaceutically acceptable salt or isomer thereof, and an agonistic composition for melanocortin receptor comprising the same as an active ingredient

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

New explortion of (S)-Tetrahydrofuran-2-carboxylic acid

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Nickel-Catalyzed Amide Bond Formation from Methyl Esters

Despite being one of the most important and frequently run chemical reactions, the synthesis of amide bonds is accomplished primarily by wasteful methods that proceed by stoichiometric activation of one of the starting materials. We report a nickel-catalyzed procedure that can enable diverse amides to be synthesized from abundant methyl ester starting materials, producing only volatile alcohol as a stoichiometric waste product. In contrast to acid- and base-mediated amidations, the reaction is proposed to proceed by a neutral cross coupling-type mechanism, opening up new opportunities for direct, efficient, chemoselective synthesis.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Discovery of 87392-07-2

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In heterogeneous catalysis, the catalyst is in a different phase from the reactants. category: Tetrahydrofurans, At least one of the reactants interacts with the solid surface in a physical process called adsorption in such a way. 87392-07-2, name is (S)-Tetrahydrofuran-2-carboxylic acid. In an article,Which mentioned a new discovery about 87392-07-2

PYRROLOTRIAZINE COMPOUNDS AND METHODS OF INHIBITING TAM KINASES

Described herein are compounds, methods of making such compounds, pharmaceutical compositions, and medicaments comprising such compounds, and methods of using such compounds to treat cancer. (II), or a pharmaceutically acceptable salt thereof, wherein: R1 is pyridin-3-yl, pyridin-4-yl, pyrazol-4-yl, cyclohexyl, or 8-azabicyclo[3.2.1]oct-2- ene-3-yl, wherein R1 is optionally substituted with up to four independently selected substituents; R2 is cyclohexyl substituted with hydroxy and optionally substituted with one or two additional substituents independently selected from C1-C4 alkyl and fluoro, or is 4,5,6,7- tetrahydro-lH-indazolyl optionally substituted with one to three substituents independently selected from C1-C4 alkyl and fluoro; and R3 is -C3-C8 alkyl, -(C2-C6 alkylene)-0-(C1-C6 alkyl), C3-C6 cycloalkyl, or -(C2-C6 alkylene)-C3-C6 cycloalkyl, wherein R3 is optionally substituted with 1-5 substituents inde endentl selected from deuterium, halo, and -OH.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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An optical pure 2 – tetrahydrofurfuryl acid preparation process (by machine translation)

The invention discloses an optical pure 2 – tetrahydrofurfuryl acid preparation process, it will L – phenylalaninol and (RS)- 2 – tetrahydrofurfuryl acid in an organic solvent in the 1st splitting obtained after reaction diastereoisomer salt, then re-crystallization (S)- 2 – tetrahydrofurfuryl acid crude product, the crude product obtained after treatment of high optical purity (S)- 2 – tetrahydrofurfuryl acid, its ee value>99%; combined split mother liquor and recrystallization of the mother liquor, containing the (R)- 2 – tetrahydrofurfuryl acid mixed solution of the, then in the mixed solution of (R)- 2 – tetrahydrofurfuryl acid with D – phenylalaninol reaction into a salt, said salt by re-crystallization (R)- 2 – tetrahydrofurfuryl acid crude product, crude product after treatment to obtain the high optical pure (R)- 2 – tetrahydrofurfuryl acid, its ee value>99%. The invention to optical pure c serinol two configuration effectively split the 2 – tetrahydrofurfuryl acid, respectively shall be 2 – tetrahydrofurfuryl acid of the two kinds of optical isomers, its ee value is greater than 99%, secondly this invention is adopted as the solvent is cheap and low boiling point of acetone, ethyl acetate and the like solvent, are used as the split reaction and re-crystallization of the solvent, the solvent is easy to recovery and high recovery rate. (by machine translation)

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

Extracurricular laboratory:new discovery of (S)-Tetrahydrofuran-2-carboxylic acid

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Substituted Pyrrolidines and Methods of Use

The invention discloses compounds of Formula (I) wherein R1, R2, R2A, R3, R3A, R4, and R5 are as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Libraries of bisdiazaphospholanes and optimization of rhodium-catalyzed enantioselective hydroformylation

Twelve chiral bis-3,4-diazaphospholane ligands and six alkene substrates (styrene, vinyl acetate, allyloxy-tert-butyldimethylsilane, (E)-1-phenyl-1,3- butadiene, 2,3-dihydrofuran, and 2,5-dihydrofuran) probe the influence of steric bulk on the activity and selectivity of asymmetric hydroformylation (AHF) catalysts. Reaction of an enantiopure bisdiazaphospholane tetraacyl fluoride with primary or secondary amines yields a small library of tetracarboxamides. For all six substrates, manipulation of reaction conditions and bisdiazaphospholane ligands enables state-of-the-art performance (90% or higher ee, good regioselectivity, and high turnover rates). For the nondihydrofuran substrates, the previously reported ligand, (S,S)-2, is generally most effective. However, optimal regio- and enantioselective hydroformylation of 2,3-dihydrofuran (up to 3.8:1 alpha-isomer/beta-isomer ratio and 90% ee for the alpha-isomer) and 2,5-dihydrofuran (up to <1_30 alpha-isomer/beta- isomer ratio and 95% ee for the beta-isomer) arises from bisdiazaphospholanes containing tertiary carboxamides. Hydroformylation of either 2,3- or 2,5-dihydrofuran yields some of the beta-formyl product. However, the absolute sense of stereochemistry is inverted. A stereoelectronic map rationalizes the opposing enantiopreferences Note that a catalyst decreases the activation energy for both the forward and the reverse reactions and hence accelerates both the forward and the reverse reactions.Application In Synthesis of (S)-Tetrahydrofuran-2-carboxylic acid, you can also check out more blogs about87392-07-2

Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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Palladium-catalyzed asymmetric coupling cyclization of terminal gamma-allenols with aryl iodides

A Pd-catalyzed asymmetric coupling cyclization of gamma-allenols has been developed. Styrenyl derivatives can be prepared in 60-86% yields with ee values ranging from 85-92%.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem

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NOVEL COMPOUNDS

The preseent invention relates to novel retinoid-related orphan receptor gamma(RORgamma)modulators and their use in the treatment ofdiseases mediated by RORgamma.

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Reference:
Tetrahydrofuran – Wikipedia,
Tetrahydrofuran | (CH2)3CH2O – PubChem