Montserrat Pérez

Stereospecific preparation of ethyl (E) and (Z)-3-aryl-e-phenylpropenoates by heck reaction

Abstract Ethyl cinnamate reacts with several para -substituted aryl iodides under Jeffery-Larock conditions (Pd(OAc) 2 , NaHCO 3 , n -Bu 4 NBr, DMF, Δ) to give ethyl ( E )-3-aryl-3-phenylpropenoates as major compounds. The reaction of para -substituted ethyl cinnamates with iodobenzene under analogous conditions affords the corresponding Z isomers. The initially stereodefined alkene formed under Heck conditions undergoes a slow isomerization.

FeCl3-catalyzed conjugate addition of secondary amines, imidazole and pyrazole to methyl 2-acetamidoacrylate. Preparation of β-dialkylamino-αalanine and β-(N-heteroaryi)-α-alanine derivatives

Abstract β-Dialkylamino-α-alanine and β-(N-heteroaryl)-α-alanine derivatives are obtained by conjugate addition of nitrogen based nuclcophiles (cyclic and acyclic secondary amines, imidazole and pirazole) to methyl 2-acetamidoacrylate, 1, under iron(III) chloride catalysis.

Prevalencia y características del síndrome metabólico en la población hipertensa española

BACKGROUND AND OBJECTIVE: Metabolic syndrome (MS) constitutes a risk factor for the development of both type 2 diabetes and cardiovascular disease. The aim of the present study was to assess the prevalence and clinical characteristics of metabolic syndrome in a sample of the hypertensive population. PATIENTS AND METHOD: Cross-sectional epidemiological study in 19,039 hypertensive patients attended in primary care centres. MS was defined using the National Education Cholesterol Program (NCEP) and the International Diabetes Federation (IDF) criteria. RESULT: The 44.6% of patients presented MS using NCEP criteria. This proportion rose to 61.7% when IDF criteria were applied. Compared with hypertensives without MS, those who fulfilled criteria were significantly (p < 0.0001) older, more frequently women, had higher blood pressure values, a poorer blood pressure control (14.4% vs 27.8%) despite the use of more antihypertensive drugs, and suffered more frequently of cardiovascular disease. Other significant abnormalities included higher serum total cholesterol, uric acid, and a decreased estimated glomerular filtration rate. CONCLUSIONS: MS is present in almost half of an unselected hypertensive population (two thirds using the newest criteria). It is more frequent in women than in men and it is associated with mild abnormalities in renal function. MS patients are more refractory to antihypertensive treatment, even with a higher number of antihypertensive drugs.

Palladium-catalyzed allylation of 3-hydroxyisoxazole, 5-isoxazolone and 5-pyrazolone Systems

Abstract Kinetic vs . thermodynamic control and steric hindrance are factors that determine the regioselectivity of the Pd(O)-catalyzed allylation of ambident heterocycles of the 3-hydroxyisoxazole, 5-isoxazolone and 5-pyrazolone series.

Palladium(0)-catalysed allylation of uracils and thiouracils. Influence of the solvent on the regioselectivity of the allylation

Abstract Uracil and 5-substituted uracils are monoallylated at N-1 in H2O-CH3CN with the catalytic systemPd(OAc) 2 P(C 6 H 4 -m- SO 3 Na ) 3 (or tppts) although performing the reaction in H2O/THF with the system Pd 2 ( dba ) 3 dppb leads to diallylations at N-1 + N-3. 2-Thiouracil, 5-methyl-2-thiouracil (2-thiothymine) and 6-methyl-2-thiouracil are monoallylated at sulfur in H 2 O CH 3 CN with the catalytic system Pd(OAc) 2 P(C 6 H 4 -m- SO 3 Na) 3 (or tppts). Performing the reactions in H2O/THF with the system Pd 2 (dba) 3 dppb leads to diallylations at N-1 + N-3 of 2-thiouracil and 2-thiothymine whereas 6-methyl-2-thiouracil is diallylated at S + N−3.

Mejoría clínica y anatomopatológica de la psoriasis en pacientes con artrosis tratados con condroitín sulfato: descripción de 3 casos

Fundamento y objetivo Con la prescripcion de condroitin sulfato como tratamiento sintomatico de la artrosis de rodilla, se observo que algunos pacientes con psoriasis concomitante mejoraban notablemente de las lesiones cutaneas. Describimos los resultados clinicos y anatomopatologicos correspondientes a las placas eritematodescamativas e hiperqueratosicas de 3 pacientes con gonartrosis y psoriasis tratados con condroitin sulfato. Pacientes y metodo Tres pacientes adultos con gonartrosis bilateral y psoriasis de larga evolucion,caracterizada por grandes placas eritematosas, descamativas e hiperqueratosicas y rebeldes a diversos tratamientos, recibieron 800 mg/dia de condroitin sulfato durante 2 meses. Seobtuvieron biopsias cutaneas antes y despues del tratamiento. Resultados En los 3 pacientes se observaron, coincidiendo con una notable mejoria clinica,una disminucion del espesor de la epidermis (espesor total, espesor desde la capa basal hasta el inicio de la cornea y espesor de la capa cornea), una disminucion del numero de queratinocitos en fase de proliferacion, una disminucion del grado de actividad de la psoriasis y la sustitucion de extensas areas de paraqueratosis por una queratinizacion ortoqueratosica. Conclusiones La administracion de condroitin sulfato consiguio una notable mejoria clinica e histologica de las lesiones psoriasicas. La confirmacion de estos resultados preliminares en futuros ensayos clinicos podria suponer un importante avance en el arsenal terapeutico para los pacientes con psoriasis, dado el excelente perfil de seguridad de este farmaco.