[structure: see text] The total synthesis of the proposed structure for spirofungin B (2) is described. The data for the synthetic material did not compare with that for the natural product leading to the conclusion that the structure 2 assigned for spirofungin B is incorrect. Analysis of the NMR data reported for spirofungins A and B as well as related spiroketals allowed for the reassignment of the stereochemistry of spirofungin B to be that corresponding to 15-epi-spirofungin A (27). 相似文献
The synthesis and isolation of the intermediates N-[1-aryl(alkyl)-3-oxo-4,4,4-trichloro-1-buten-1-yl]-o-phenylenediamines 2a-f and the corresponding 2-trichloromethyl-4-aryl-3H-1,5-benzodiazepines 3c-g or benzimidazoles 4a-b derivatives obtained from the intramolecular cyclization of 2a-f or from direct cyclo-condensation reaction of β-alkoxyvinyl trichloromethyl ketones 1a-g with o-phenylenediamine, is reported. Depending of the structure of the β-alkoxyvinyl trichloromethyl ketones or the N-[1-aryl(alkyl)-3-oxo-4,4,4-trichloro-buten-1-yl]-o-phenylenediamines and the reactions conditions, benzimidazoles or 3H-1,5-benzodiazepines were obtained. 相似文献
Bone histomorphometry or quantitative histology consists of counting or measuring tissue components: cells, extracellular constituents and microarchitecture. Bone histomorphometry is the only method that allows the measurement of mineralization rate and the study of bone formation at three levels: cell, remodeling unit and tissue levels. It is a useful tool to explain the pathogenesis and cellular mechanisms of different metabolic bone diseases such as glucocorticoid-induced osteoporosis (GIO).
Glucocorticoids (GC) affect calcium and bone metabolism at every level, but the main effect is the osteoblastic dysfunction.
Concerning the bone formation, some histomorphometric studies have shown a depressed osteoblastic activity at a cell, bone remodeling unit, and tissue levels. In addition, there is evidence of a shortening of the period in which the osteoblasts work actively forming the bone matrix. This latter effect seems to occur after high cumulative doses of GC. With regard to the resorption, the results are still debated, but histomorphometric parameters seem to be increased in the majority of studies, at least in the first period of the GC treatment. From a structural point of view, GC seem to induce a thinning of the trabeculae without their perforation, which occurs only after high cumulative doses. Antiresorptive treatments, such as bisphosphonates, are able to counteract the negative effects of GC on bone. In particular, along with their active working period, they prolong the lifespan of osteoblasts and osteocytes. In addition, the antiresorptive treatments seem to extend the time for secondary mineralization through a reduction of the Activation Frequency. The latter is an intriguing mechanism of bisphosphonates in GIO that needs further ad hoc investigations. 相似文献
This paper describes an efficient approach for the synthesis of a new series of 6‐[3‐alkyl(aryl/heteroaryl)‐5‐trifluoromethyl‐1H‐pyrazol‐1‐yl]nicotinic acids (where alkyl = CH3; aryl = Ph, 4‐OCH3Ph, 4,4′‐BiPh; and heteroaryl = 2‐Furyl) from the hydrolysis reaction of alkyl(aryl/heteroaryl)substituted 2‐(5‐trifluoromethyl‐5‐hydroxy‐4,5‐dihydro‐1H‐pyrazol‐1‐yl)‐5‐(5‐trifluoromethyl‐5‐hydroxy‐4,5‐dihydro‐1H‐1‐carbonylpyrazol‐1‐yl)pyridines, under basic conditions and at 70–95% yields. In a subsequent step, the esterification reaction of pyrazolyl‐nicotinic acids done in thionyl chloride and methanol led to the isolation of a series of methyl 6‐[alkyl(aryl/heteroaryl)‐5‐trifluoromethyl‐1H‐pyrazol‐1‐yl] nicotinates as stable hydrochloride salts at 64–84% yields, which could be easily converted to hydrazides to give new oxadiazolyl‐pyrazolyl‐pyridine tricyclic scaffolds at good yields from a [4 + 1] cyclocondensation reaction with 1,1,1‐triethoxyethane and 1‐(triethoxymethyl)benzene as the reagent/solvent. 相似文献
A series of 10 heterocycles was obtained from the reaction of 1,1,1-trifluoro-4,4-diethoxy-3-buten-2-one and 1,1,1,2,2-pentafluoro-4,4-diethoxy-3-penten-2-one with different dinucleofiles (hydrazine, methyl hydrazine, hydroxylamine and sodium cyanide). The pyrazoles, 4,5-dihydroisoxazoles and pyrrolidinones polyfluoroalkyl substituted were obtained in moderate to good yields under mild conditions. 相似文献
We report herein the synthesis of cytotoxic cyanobactin, Wewakazole B through an efficient solution-phase approach. The key steps of the synthesis are the macrocyclic lactamization of linear dodecapeptide and construction of two hexapeptides with three different substituted oxazole rings. 相似文献
Pyrazolo[1,5-a]pyrimidines were synthesized via the ultrasonic sonochemical method using the cyclocondensation reaction of 4-alkoxy-1,1,1-trifluoro-3-alken-2-ones [CF3C(O)CH = C(R)(OMe) – where R = Me, Bu, i-Bu, Ph, 4-Me–C6H4, 4-F–C6H4, 4-Cl–C6H4, 4-Br–C6H4, naphth-2-yl and biphen-4-yl] – with 3-amino-5-methyl-1H-pyrazole in the presence of EtOH for 5 min. This methodology has several advantages, for example, it is a simple procedure, it has an easy work-up, mild conditions, short reaction times (5 min) and produces satisfactory yields (61–98%). 相似文献
A microwave-assisted synthesis of a series of 1-aryl-4-dimethylaminomethylene pyrrolidine-2,3,5-triones from the cyclocondensation reaction of ethyl 5,5,5-trichloro-3-dimethylamino methylene-2,4-dioxopentanoate with aniline, 3- or 4-substituted anilines [where the substituents = 3-Me, 3-OMe, 3-OH, 4-Me, 4-F, 4-Cl, 4-Br, 4-NO2, and 4-COMe] is reported. This process is an efficient alternative to the conventional thermal heating and furnishes the products in a short reaction time (ca. 13 min), under mild conditions and in moderate to good yields (50–76%). 相似文献
We present a detailed Raman scattering study of the boson peak evolution in vitreous silica as a function of density, from the normal one up to ~ 22% of densification. We show that the distribution of low frequency modes in the boson peak range does not change as a function of density, at least until the densification process starts to modify the glassy network structure from a fourfold coordinated structure into a sixfold coordinated one. 相似文献