KETOCONAZOLE 2S 4R

KETOCONAZOLE 2S 4R

ALSO

142128-57-2
228850-16-6 (tartrate)

(-)-cis-1-Acetyl-4-[4-[2(S)-(2,4-dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolan-4(R)-ylmethoxy]phenyl]piperazine

531.431, C26 H28 Cl2 N4 O4

COR-003
DIO-902
LDKTZ

CORTENDO

licensee DiObex

Example 14 : (2S,4R)-(-)-1-acetyl-4-[4-[ [2-(2,4-dichlorophenyl)-2-[(1H-imidazol-1-yl)-methyl]-1,3-dioxolane-4-yl]methoxy]phenyl]piperazine, (2S,4R) -(- )-ketoconazole.

This compound is prepared following the process described above for (2R,4S)-(+)-ketoconazole. Starting from HNa (60-65% dispersion in paraffin, 32 mg, 0.80 mmol), 1-acetyl-4-(4-hydroxyphenyl)piperazine (153 mg, 0.69 mol) and (2S,4S)-(-)-IV (Ar = 2,4-dichlorophenyl, Y = CH, R = CH3) (250 mg, 0.61 mmol), upon crystallization from an acetone:ethyl acetate mixture, (2S,4R) -(-)-ketoconazole is obtained [(2S,4R)-V Ar = 2,4-dichlorophenyl, Y = CH, Z = COCH3] (196 mg, 61% yield) as a solid, m.p. 153-155ºC (lit. 155-157ºC); [α]D 20 = -10.50 (c = 0.4, CHCl3) (lit. [α]D 25 = -10.58. c = 0.4, CHCl3) with e.e. > 99% (determined by HPLC using the chiral stationary phase CHIRALCEL OD-H and ethanol:hexane 1:1 mixtures containing 0.1 % diethylamine as the eluent).

 http://www.google.com/patents/WO1996029325A1?cl=en
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Andaman and Nicobar Islands - Wikipedia, the free ...

en.wikipedia.org/wiki/Andaman_and_Nicobar_Islands

The capital of Nicobar Islands is Car Nicobar. The islands host the Andaman and Nicobar Command, the only tri-service geographical command of the Indian ...

‎Port Blair - ‎Car Nicobar - ‎Cellular Jail - ‎2014 Andaman boat disaster

 


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Lost Tribe On Small Island In The Indian Ocean remain virtually untouched by modern civilization

The Sentinelese (also Sentineli, Senteneli, Sentenelese, North Sentinel Islanders) are one of the Andamanese indigenous peoples and one of the most uncontacted peoples of the Andaman Islands, located in India in the Bay of Bengal. They inhabit North Sentinel Island which lies westward off the southern tip of the Great Andaman archipelago. They are noted for vigorously resisting attempts at contact by outsiders. The Sentinelese maintain an essentially hunter-gatherer society subsisting through hunting, fishing, and collecting wild plants; there is no evidence of either agricultural practices or methods of producing fire. Their language remains unclassified.

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The present population of the Sentinelese is not known with any great degree of accuracy. Estimates have been produced ranging from lower than 40, through a median of around 250, and up to a maximum of 500. In the year 2001, the Census of India officials recorded 39 individuals (21 males and 18 females); however, out of necessity this survey was conducted from a distance and almost certainly does not represent an accurate figure for the population who range over the 72 km² (17,800 acres) island. Any medium- or long-term impact on the Sentinelese population arising from the 2004 Indian Ocean earthquake and resulting tsunami remains unknown, other than the confirmation obtained that they had survived the immediate aftermath.
On previous visits, groups of some 20–40 individuals were encountered regularly. Habitations of 40–60 individuals were found on two occasions. As some individuals are almost certainly hiding, a better approximation of group size cannot be determined. This would suggest that some 2–6 groups occupy the island. The rule of thumb population density of 1.5 km² (370 acres)/individuals in comparable hunter-gatherer societies indicates that one such group could live off the land alone. A significant amount of food is derived from the sea. It seems that the groups encountered, at any one time, could only have come from a rather small part of the island. There appear to be slightly more males than females. At any given time, about half of the couples seemed to have dependent children or the women were pregnant.

North Sentinel Island

The Sentinelese and other indigenous Andamanese peoples are frequently described as negritos, a term which has been applied to various widely separated peoples in Southeast Asia, such as the Semang of the Malay archipelago and the Aeta of the Philippines, as well as to other peoples as far afield as Australia (notably former populations of Tasmania). The defining characteristics of these “negrito” peoples (who are not a monophyletic group) include a comparatively short stature, dark skin and “peppercorn” hair, qualities also found commonly across the continent of Africa. No close contacts have been established, but the author Heinrich Harrer described one man as being 1.6 m (5′ 4″) tall and apparently left handed.

Negrito people of the Andaman Islands

From 1967 onwards, the Indian authorities in Port Blair embarked on a limited program of attempts at contacting the Sentinelese, under the management of the Director of Tribal Welfare and anthropologist T. N. Pandit. These “Contact Expeditions” consisted of a series of planned visits which would progressively leave “gifts”, such as coconuts, on the shores, in an attempt to coax the Sentinelese from their hostile reception of outsiders. For a while, these seemed to have some limited success; however, the program was discontinued in the late 1990s following a series of hostile encounters resulting in several deaths.

In 2006, Sentinelese archers killed two fishermen who were fishing illegally within range of the island. The archers later drove off, with a hail of arrows, the helicopter that was sent to retrieve the bodies.  To this date, the bodies remain unrecovered, although the downdraft from the helicopter’s rotors at the time exposed the two fishermen’s corpses, which had been buried in shallow graves by the Sentinelese.

On 2 August 1981, the ship Primrose grounded on the North Sentinel Island reef. A few days later, crewmen on the immobile vessel observed that small black men were carrying spears and arrows and building boats on the beach. The captain of the Primrose radioed for an urgent airdrop of firearms so the crew could defend themselves, but did not receive them. Heavy seas kept the islanders away from the ship. After a week, the crew were rescued by a helicopter working under contract to the Indian Oil And Natural Gas Commission (ONGC).
The Sentinelese apparently survived the 2004 Indian Ocean earthquake and its after-effects, including the tsunami and the uplifting of the island. Three days after the event, an Indian government helicopter observed several of them, who shot arrows and threw stones at the hovering aircraft with the apparent intent of repelling it. Although the fishing grounds of the Sentinelese were disturbed, they appear to have adapted to the island’s current conditions.