We report an efficient kinetic resolution of racemic 2-(4-chlorophenyl)-4-hydroxytetrahydro-pyran (CLP-4-HTHP) via Pseudomonas cepacia lipase (PSL)-catalyzed transesterification, where PSL is immobilized on a core–shell MnFe2O4@SiO2-(CH2)3-NH2 carrier and used as a magnetically separable cataly...

(S)-1-(2-chlorophenyl)ethanol is a key intermediate of L-cloprenaline used for relieving asthma symptoms. The asymmetric reduction of 2-chloroacetophenone 1 to (S)-1-(2-chlorophenyl)ethanol 2 in the submerged culture of Alternaria alternata isolates was studied. A. alternata EBK-8 isolate was th...

We report herein on bioprocess development guided by the hydrophobicities of substrate and product. Bioreductions of o-chloroacetophenone are severely limited by instability of the catalyst in the presence of aromatic substrate and (S)-1-(2-chlorophenyl)ethanol. In situ substrate supply and prod...

(R)-2-Chloro-1-(m-chlorophenyl)ethanol, a precursor of (R)-3-chlorostyrene oxide which is the key chiral intermediate for the preparation of several β3-adrenergic receptor agonists was prepared in 40% yield and 99% ee by the Lipozyme TL IM-catalyzed second resolution of the corresponding racema...

The direct HPLC resolution of the enantiomers of methoxy and hydroxy derivatives of 3,4-dihydro-3-(dipropylamino)-2H-1-benzopyrans and of unsubstituted amino compounds was achieved using Chiralcel OD and/or Chiralpak AD stationary phases. The position of the substituent (methoxyl or hydroxyl) in...

Chiral separation of 3,4-dihydro-2H-1-benzopyran derivatives by capillary zone electrophoresis was achieved by employing β-cyclodextrin (β-CD) as chiral selector. The effects of electrolyte composition (β-cyclodextrin concentration, ionic strength and pH of the buffer) on the migration time, ...

A series of new 3-amino, 3-aminomethyl-5-alkoxy-3,4-dihydro-2H-1-benzopyran and 5′-alkoxy-3′,4′-dihydrospiro[piperazine-2,3′(2′H)-benzopyran] derivatives was prepared and evaluated for affinity at 5-HT1A, 5-HT2A and D2 receptors. Two of the compounds (Figure 3, Scheme 3, Figure 4, Scheme 4)...

Synthesis of N-substituted-3,4-dihydro-2H-1-benzopyran derivatives which have a potential affinity for the 5-HT1A receptor is reported. The comparison between the experimental values of binding and the prediction of Q.S.A.R. studies is described.

Highly enantioselective reduction of 3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-ones 3 a-e by BH3 was achieved in the presence of catalytic amounts of Corey's oxazaborolidine 4 to afford the corresponding 3,4-dihydro-2,2-dimethyl-2H-1-benzopyran-4-ols2a-e in quantitative yields. These benzo...

The present work aimed at exploring a series of diversely 4-arylthiourea-substituted R/S-3,4-dihydro-2,2-dimethyl-6-halo-2H-1-benzopyrans structurally related to (±)-cromakalim. These new compounds were examined in vitro as putative potassium channel openers (PCOs) on rat pancreatic islets (inh...

Objective: The purpose of this study is to evaluate the validity and reliability of scintimammography with technetium-99m (99mTc)-labeled sestamibi as an adjunct radiodiagnostic agent in the diagnosis of breast cancer.Methods: This is a multicenter prospective cohort clinical trial that was init...

IntroductionTechnetium-99m–sestamibi (MIBI) is the most frequently used myocardial perfusion tracer in patients with ischemic heart disease. In patients with acute ST-elevation myocardial infarction, we previously found that the defect in myocardial MIBI uptake was the same in patients injected...

The myocardial uptake of rest-injected technetium 99m sestamibi on single-photon-emission computed tomographic images was assessed in 25 patients. All had an area of myocardial dysfunction that could be related to a coronary artery stenosis. None of the patients had clinical evidence of a myocar...

SummaryThe accurate identification of the location of hyperfunctioning parathyroid nodules is essential to the effective surgical treatment of hyperparathyroidism. Radionuclide imaging has played an important role in the detection of pathological parathyroid nodules. Sestamibi is a new radiophar...

ObjectiveTo study the clinical value of Technetium-99m sestamibi myocardial perfusion single photon emission computed tomography (SPECT) in diabetes with suspected coronary artery diseases.

We analyzed the left-ventricular functional data obtained by cardiac-gated single-photon emission computed tomography myocardial perfusion imaging (MPI) with thallium-201 (Tl-201) and technetium-99m-sestamibi (MIBI) protocols in different groups of patients, and compared the data between Tl-201 ...

BackgroundIn hyperparathyroidism, dual-phase technetium-99m sestamibi scintigraphy is important for parathyroid adenoma localization. We hypothesized that reviewing early-phase scans can increase localization in patients with primary hyperparathyroidism (PHPT).

BackgroundParathyroidectomy for patients with secondary hyperparathyroidism (sHPT) generally requires a four-gland exploration. Some groups have strongly recommended routine preoperative Tc-99m-sestamibi scans; others practice scanning for only selected patients. To determine the utility of sest...

BackgroundInterest in technetium-99m (99mTc)-sestamibi imaging for neoadjuvant chemotherapy (NAC) response monitoring in locally advanced breast cancer (LABC) is increasing but remains matter of discussion. The present study conducted a meta-analysis of the diagnostic performance of 99mTc-sestam...

BackgroundMinimally invasive parathyroidectomy (MIP) is dependent upon accurate preoperative parathyroid localization. We hypothesized that surgeon recognition of subtle differences in radiotracer accumulation would increase the sensitivity of technetium-99m sestamibi imaging and result in more ...