Stereoselective Dehydroxyboration of Allylic Alcohols to Access ()-Allylboronates by a Combination of C-OH Cleavage and Boron Transfer under Iron Catalysis.

Iron-catalyzed direct S2' dehydroxyboration of allylic alcohols has been developed to access ()-stereoselective allylboronates. Allylic alcohols with diverse structures and functional groups, especially derived from natural products, underwent smooth transformation. The six-membered ring transition state formed by allylic alcohols and iron-boron intermediate was indicated to be the key component involved in transfer of the boron group, activation of the C-OH bond, and control of the stereoselectivity.

Synthesis and activity evaluation of the cyclic dipeptides arylidene N-alkoxydiketopiperazines.

A series of arylidene N-alkoxydiketopiperazines was designed and stereoselectively synthesized via oxime-ether formation and intramolecular acylation. Possible cyclization and acid-catalyzed rearrangement-fragmentation mechanisms were discussed. The crystal structure of the novel diketopiperazine further confirmed the rearrangement mechanism.

Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.

A series of open-chain analogs of cyclic peptides was designed and synthesized using sansalvamide A as a model compound. All compounds exhibited low antitumor activity. Furthermore, the evaluation of their inhibitory potency toward IMPDH, SHP2, ACHE, proteasome, MAGL, and cathepsin B showed that all of the compounds were potent against protein tyrosine phosphatase Shp2.

3-(3,4-Dihydroxyphenyl)-1-methoxy-1-oxopropan-2-aminium chloride.

In the title compound, C(10)H(14)NO(4) (+)·Cl(-), the benzene ring makes a dihedral angle of 64.68 (4)° with the methyl-amino-propano-ate unit, which is bonded to the catechol ring via a methyl-ene C atom. A strong intra-molecular O-H⋯O hydrogen bond occurs.

(Anthracen-9-ylmeth-yl)benzyl-ammonium chloride.

In the title compound, C(22)H(20)N(+)·Cl(-), the anthracene system makes a dihedral angle of 72.65 (4)° with the benzene ring. The C-N-C-C torsion angles in the chain connecting the benzene ring and anthracene system are 52.

Dimethyl 2-(2,4,6-trimethoxy-benz-yl)malonate.

In the title compound, C(15)H(20)O(7), the benzene ring makes dihedral angles of 69.17 (5) and 80.81 (4)° with the two side chains of malonate.

Dimethyl 2-(2-quinolylmeth-yl)malonate.

In the title compound, C(15)H(15)NO(4), the quinoline ring system and one of the malonate side chains are essentially coplanar (r.m.s.

[Inhibitory effect of N-acetylcysteine upon atherosclerotic processes in rabbit carotid].

Objective: To discuss the effect of N-acetylcysteine (NAC) upon matrix metalloproteinases (MMP) in the atherosclerotic processes in rabbit carotid.

Methods: The atherosclerotic models were generated in vitro by injuring rabbit internal carotid with arterial canal balloon. These rabbits were divided into 3 groups (15 mg/kg NAC, 30 mg/kg NAC and control group) and treated for 8 weeks.

[Effects of probucol, aspirin and atorvastatin combination therapy upon atherosclerosis].

Objective: To investigate the effects of probucol, aspirin and atorvastatin (PAS) combination therapy upon atherosclerosis.

Methods: A total of 436 patients with coronary artery disease were selected and randomly divided into control group (aspirin 100 mg, atorvastatin 10 mg daily) and PAS group (aspirin 100 mg, atorvastatin 10 mg and probucol 0.25 g daily).

2,5-Bis[2-(2-methoxy-ethoxy)phen-yl]-1,3,4-oxadiazole.

In the title compound, C(20)H(22)N(2)O(5), the central 1,3,4-oxadiazole ring is essentially planar [r.m.s.

11-(p-Tolylsulfonyl)-8,14,24-trioxa-11,22,23-triazatetracyclo[19.2.1.0.0]tetracosa-1(23),2,4,6,15,17,19,21-octaene.

In the title compound, C(25)H(23)N(3)O(5)S, the central 1,3,4-oxadiazole ring makes dihedral angles of 35.05 (7), 23.68 (7) and 82.

(E)-1,5-Dimethyl-4-[3-(4-nitro-benz-yloxy)benzyl-ideneamino]-2-phenyl-1H-pyrazol-3(2H)-one.

In the title compound, C(25)H(22)N(4)O(4), the central benzene ring, makes dihedral angles of 74.35 (6), 17.01 (8) and 62.

(E)-4-[(1,5-Dimethyl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazol-4-yl)imino-meth-yl]phenyl 4-bromo-benzene-sulfonate.

In the title compound, C(24)H(20)BrN(3)O(4)S, the central benzene ring makes dihedral angles of 17.13 (13), 39.83 (13) and 58.

(E)-N'-[2-(4-Chloro-3-nitro-phenyl-sulfon-yloxy)-3-methoxy-benzyl-idene]isonicotinohydrazide acetic acid tetra-solvate.

In the title compound, C(20)H(15)ClN(4)O(7)S·4CH(3)COOH, the central o-vanillin group makes dihedral angles of 9.50 (11) and 42.86 (7)°, respectively, with its attached pyridine and nitro-benzene rings.