RESUMEN
The first total synthesis of the marine alkaloid aqabamycin G is disclosed. The synthetic sequence involved the stepwise addition to maleimide of an indole motif and a substituted diazo-benzenoid unit derived from acetaminophen. An alternative strategy using a protected phenol is also reported.
Asunto(s)
Alcaloides , Antineoplásicos , Vibrio , Acetaminofén , Maleimidas , Indoles , Fenoles , Alcaloides IndólicosRESUMEN
The broad-spectrum antiviral Remdesivir, a monophosphate nucleoside analogue prodrug (ProTide), was repurposed. In May 2020, it received emergency approval by the FDA, being the first drug approved to fight the new coronavirus (COVID-19) disease which targets the virus directly. The main synthetic strategies toward Remdesivir, and their relevant modifications, are presented and discussed, to provide a panoramic view of the state-of-the-art and the more important advances in this field. Recent progress, proposed improvements, and uses of novel technologies for the synthetic sequence are also detailed.
RESUMEN
Covering: 2006 to 2018 The application of the 6π-azaelectrocyclization of azatrienes as a key strategy for the synthesis of natural products, their analogs and related bioactive or biomedically-relevant compounds (from 2006 to date) is comprehensively reviewed. Details about reaction optimization studies, relevant reaction mechanisms and conditions are also discussed.
Asunto(s)
Alcaloides/síntesis química , Productos Biológicos/síntesis química , Técnicas de Química Sintética/métodos , Compuestos Aza/química , Ciclización , Agonistas de los Receptores Histamínicos/síntesis química , Piperidinas/química , Piridinas/química , Pirroles/síntesis química , Quinazolinas/síntesis química , Quinolizinas/química , Sesquiterpenos/síntesis químicaRESUMEN
Four boys of the same family (three first cousins and their uncle) had the same syndrome of multiple malformations. They had hypertelorism, antimongolian slant of the palpebral fissures, low-set ears, and Pierre Robin syndrome. The ossification of the skull vault was defective, with broad sutures and fontanelles. The ribs were sinuous, the clavicles were long, thin, and sloping, and the vertebrae were flattened. There were abnormal bowing with hyperostosis of the long bones, faulty ossification of the bones of hand and feet, and "fanned-out" toes. The disorder was lethal within a few weeks. The karyotype was normal. The mothers of affected boys had a mild form of the same abnormal facies. Transmission of this disorder appears to be linked to the X chromosome.
Asunto(s)
Anomalías Múltiples/genética , Fisura del Paladar/genética , Disostosis Craneofacial/genética , Cara/anomalías , Hipertelorismo/genética , Síndrome de Pierre Robin/genética , Huesos/anomalías , Huesos/diagnóstico por imagen , Femenino , Humanos , Lactante , Recién Nacido , Masculino , Linaje , Síndrome de Pierre Robin/diagnóstico por imagen , Radiografía , Cromosoma XRESUMEN
Resection of the achalasic area and replacement by a segment of jejunal loop, associated with vagotomy and pyloroplasty, has been performed in 21 patients. The majority of these patients had Chagas' disease, with a dilated esophagus wider than 7 cm. This surgical procedure offered symptomatic relief in 20 of our 21 cases. One patient died, but the death was not necessarily related to the operation. Although disphagia and regurgitation did not disappear entirely in all cases the decrease in severity of these symptoms was such to allow the few symptomatic patients to lead an entirely normal life after the operation.