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An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles.

ABSTRACT: This review which is the second in this series summarises the most common synthetic routes as applied to the preparation of many modern pharmaceutical compounds categorised as containing a six-membered heterocyclic ring. The reported examples are based on the top retailing drug molecules combining synthetic information from both scientific journals and the wider patent literature. It is hoped that this compilation, in combination with the previously published review on five-membered rings, will form a comprehensive foundation and reference source for individuals interested in medicinal, synthetic and preparative chemistry.

SUBMITTER: Baumann M

PROVIDER: S-EPMC3817479 | biostudies-literature | 2013 Oct

REPOSITORIES: biostudies-literature

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An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles.

Baumann Marcus M Baxendale Ian R IR

Beilstein journal of organic chemistry 20131030

This review which is the second in this series summarises the most common synthetic routes as applied to the preparation of many modern pharmaceutical compounds categorised as containing a six-membered heterocyclic ring. The reported examples are based on the top retailing drug molecules combining synthetic information from both scientific journals and the wider patent literature. It is hoped that this compilation, in combination with the previously published review on five-membered rings, will ...[more]

PMID: 24204439

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Project description:ImportanceBecause moisturizer use is critical for the prevention and treatment of numerous dermatological conditions, patients frequently request product recommendations from dermatologists.ObjectiveTo determine the product performance characteristics and ingredients of best-selling moisturizers.Design and settingThis cohort study involved publicly available data of the top 100 best-selling whole-body moisturizing products at 3 major online retailers (Amazon, Target, and Walmart). Products marketed for use on a specific body part (eg, face, hands, eyelids) were excluded.Main outcomes and measuresPairwise comparisons of median price per ounce on the basis of marketing claims (eg, dermatologist recommended, fragrance free, hypoallergenic) and presence of ingredients represented in the North American Contact Dermatitis Group (NACDG) series were conducted using Wilcoxon rank sum tests. The effect of vehicle type (eg, ointment, lotion, cream, butter) was assessed using the Kruskal-Wallis test. Cross-reactors and botanicals for fragrances were derived from the American Contact Dermatitis Society's Contact Allergen Management Program database.ResultsA total of 174 unique best-selling moisturizer products were identified, constituting 109 713 reviews as of August 2016. The median price per ounce was $0.59 (range, $0.10-$9.51 per ounce) with a wide range (9400%). The most popular vehicles were lotions (102 [59%]), followed by creams (22 [13%]), oils (21 [12%]), butters (14 [8%]), and ointments (3 [2%]). Only 12% (n = 21) of best-selling moisturizer products were free of NACDG allergens. The 3 most common allergens were fragrance mix (n = 87), paraben mix (n = 75), and tocopherol (n = 74). Products with the claim "dermatologist recommended" had higher median price per ounce ($0.79; interquartile range [IQR], $0.56-$1.27) than products without the claim ($0.59; IQR, $0.34-$0.92). Products with the claim "phthalate free" had higher median price per ounce ($1.38; IQR, $0.86-$1.63) than products without the claim ($0.59; IQR, $0.35-$0.91). Lotions (median, $0.49; IQR, $0.31-0.68) were statistically less expensive per ounce than butters (median, $1.20; IQR, $0.76-$1.63), creams (median, $0.80; IQR, $0.69-$1.25) and oils (median, $1.30; IQR, $0.64-$2.43). For products with a claim of "fragrance free," 18 (45%) had at least 1 fragrance cross-reactor or botanical ingredient. Products without any ingredients in the NACDG (median, $0.83; IQR, $0.47-$1.69) were not statistically more expensive per ounce than products with 1 or more allergens (median, $0.60; IQR, $0.35-$1.06).Conclusions and relevanceBest-selling moisturizers vary widely by price and product characteristics. Given the lack of readily available comparison data on moisturizer efficacy, dermatologists should balance consumer preference, price, and allergenicity in their recommendations.

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An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles.

Publications

An overview of the synthetic routes to the best selling drugs containing 6-membered heterocycles.

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